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One-pot,Catalytic Asymmetric Reductive Bischler–Napieralski-Type Reaction of Amides:An Enantioselective Entrance to Biologically Active 1-Substituted Tetrahydroisoquinolines 认领 引用
1
作者 Lu Guangsheng Han Zeng +1 位作者 Ye Jianliang Huang Peiqiang 《化学学报》 SCIE CAS CSCD 北大核心 2026年第4期476-483,共8页
Herein,we report the one-pot,catalytic asymmetric reductive Bischler-Napieralski-type reaction of amides as the first demonstration of a new strategy for the asymmetric reductive transformation of amides,which allowed... Herein,we report the one-pot,catalytic asymmetric reductive Bischler-Napieralski-type reaction of amides as the first demonstration of a new strategy for the asymmetric reductive transformation of amides,which allowed for the one-pot,enantioselective access to tetrahydroisoquinoline(THIQ).The method features a tandem sequence involving the Tf2O/2-F-Pyr.-promoted Bischler-Napieralski dehydracyclization and an aqueous Noyori-type catalytic asymmetric transfer hydrogenation(CATH).By this one-pot method,a variety of THIQ derivatives were synthesized in high yields and in excellent enantioselectivities.This protocol accommodates N-arylethyl aromatic amides bearing either electron-donating or electron-withdrawing groups on the acyl moiety,and N-arylethyl aliphatic amides.The synthetic utility of this methodology was demonstrated via the efficient,catalytic enantioselective synthesis of four alkaloids:(S)-salsolidine,(S)-laudanosine,(S)-xylopinine,and(S)-N-norlaudanidine,and medicinal agent ACT-335827.Additionally,formal syntheses of alkaloid(S)-cryptostyline III and medicinal agents such as almorexant were achieved. 展开更多
关键词 amides amide activation tetrahydroisoquinolines alkaloids reductive Bischler-Napieralski-type reaction catalytic asymmetric transfer hydrogenation catalytic asymmetric synthesis
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Enantioconvergent reductive amidation of benzyl ammonium salts for synthesis of α-chiral amides 认领 引用
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作者 Saima Perveen Xicheng Wang +6 位作者 Tao Li Linghua Wang Shuai Zhang Yizhao Ouyang Xue Zhao Liang Xu Pengfei Li 《Chinese Chemical Letters》 SCIE CAS CSCD 2026年第1期300-305,共6页
α-Chiral amides are common in pharmaceuticals,agrochemicals,natural products,and peptides,prompting the need for new synthetic methods.Here,we introduce a nickel-catalyzed asymmetric reductive amidation method to syn... α-Chiral amides are common in pharmaceuticals,agrochemicals,natural products,and peptides,prompting the need for new synthetic methods.Here,we introduce a nickel-catalyzed asymmetric reductive amidation method to synthesizeα-chiral amides from benzyl ammonium salts and isocyanates.The key to success is using a chiral 2,2-bipyridine ligand(-)-Ph-SBpy,enabling high yield(up to 95%)and enantiomeric ratio(up to 98:2 er)under mild conditions.Addition of phenol prevents isocyanate polymerization by reversibly forming a carbamate intermediate,enhancing selectivity and efficiency.The synthetic utility is showcased through transformations of the enantioenriched amides,and the mechanism and enantioselectivity are supported by experimental and computational studies. 展开更多
关键词 α-Chiral amide Amidation Asymmetric synthesis Bipyridine ligand Nickel catalysis
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Electro-oxidation synthesis of amides from carbon-and nitrogen-containing small molecules 认领 引用
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作者 Aijing Ma Baian Shen +2 位作者 Minghao Guo Chengying Guo Yifu Yu 《Chinese Journal of Catalysis》 SCIE EI CAS CSCD 2026年第1期1-6,共6页
Electrochemical synthesis of amides from carbon-and nitrogen-containing small molecules is alluring from the view of carbon neutrality.Previous works were mainly focused on electro-reduction coupling of C-N bond to pr... Electrochemical synthesis of amides from carbon-and nitrogen-containing small molecules is alluring from the view of carbon neutrality.Previous works were mainly focused on electro-reduction coupling of C-N bond to prepare amides coupled with the useless oxygen evolution reaction on the anode.But,the competing hydrogen evolution reaction is more favorable in dynamics on the cathode,severely retarding the Faradaic efficiency of the amides.Very recently,electro-oxidation construction of C-N bond via coupling the cheap C-and N-containing small molecules to achieve high energy efficiency emerges as a rising star,while the big challenge lies in preventing the sole oxidation of feedstocks.In this perspective,we highlight the recent progress in anodic electro-oxidation synthesis of amides and the potential reaction mechanism.We also discuss the application potential and the development opportunities of the electro-oxidation strategy for amides synthesis from carbon-and nitrogen-containing small molecules. 展开更多
关键词 Amides Electrosynthesis Oxidation coupling C-N bond Sustainable feedstocks
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Amide-bonded superhydrophilic heterojunction for efficient photothermal catalysis toward hydrogen generation and pollutant degradation via multiple charge transfer pathways 认领 引用
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作者 Weiwei Sun Xuyang Hu +4 位作者 Xinyuan Chu Jiapeng Pan Qingzheng Tian Lina Yang Zhenjiang Li 《Journal of Energy Chemistry》 SCIE EI CAS CSCD 2026年第7期446-461,I0012,共16页
The recently emerging heterojunctions with remarkable thermal effects and chemical bonding have attracted intensive attention due to their fast photocarrier separation and transportation.Herein,quasizero-dimensional c... The recently emerging heterojunctions with remarkable thermal effects and chemical bonding have attracted intensive attention due to their fast photocarrier separation and transportation.Herein,quasizero-dimensional carbon quantum dot(0D CQD)with multi-functional groups is adopted to in situ construct a superhydrophilic heterojunction on electron-deficient Se-doped ZnCdS(Se-ZCS)via amide linkages.Sulfur vacancies in Se-ZCS serve as electron reservoirs,and photothermally active CQD function as hydrophilic components,light capturers,and electron acceptors,while the amide bond channels promote the smooth carrier transfer across the Se-ZCS/CQD interface.Simultaneously,the interfacial electronic barrier prohibits the photoelectron transfer to Se-ZCS.Thereby,the formed Se-ZCS/CQD heterojunction successfully elongates the photoelectron lifetime to drive efficient photothermal catalytic reactions.Particularly,optimal Se-ZCS/CQD achieves a 2-fold increase in H2 production(126.8 mmol gcat-1h-1)compared to pure Se-ZCS under visible light irradiation,surpassing the majority of reported ZnCdSbased photocatalysts.More importantly,it exhibits exceptional long-term stability with only a decline of 8.07%after 16 h of testing.The expanded application of Se-ZCS/CQD in the pretreatment of wastewater presents a removal efficiency of~96.5%after 2 h.The strategy provides a new idea for designing chemical contact between semiconductor and photothermal active materials,and for realizing efficient photocatalysis by improving charge separation and transfer. 展开更多
关键词 Interfacial amide bond Superhydrophilic heterojunction Polarization electric field ZnCdS Carbon quantum dot
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Non-coordinating solvent anchoring strategy regulated fluorinated amide electrolyte for ultrahigh-rate and high-voltage Li metal batteries 认领 引用
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作者 Yilu Wu Qinghui Zhang +1 位作者 Daize Mo Kuirong Deng 《Journal of Energy Chemistry》 SCIE EI CAS CSCD 2026年第3期106-115,共10页
High-voltage Li metal batteries hold great promise for next-generation energy storage,but constructing robust and highly conductive electrode/electrolyte interfaces via electrolyte engineering to enhance the battery p... High-voltage Li metal batteries hold great promise for next-generation energy storage,but constructing robust and highly conductive electrode/electrolyte interfaces via electrolyte engineering to enhance the battery performance is still a challenge.Herein,we propose a non-coordinating solvent anchoring strategy to regulate fluorinated amide electrolyte to enhance the stability and ionic conductivity of the interfaces.Specifically,hexafluorobenzene is employed to anchor fluorinated amide solvent by the robust dipole–dipole interactions,which weaken the coordination between fluorinated amide and Li+,facilitate more anions coordinating with Li+,and form more ion aggregates.Consequently,stable and highly conductive electrode/electrolyte interfaces enriched with LiF and Li3N are constructed,drastically improving the interfacial stability and reducing interface impedance of Li metal anodes and LiNi0.8Co0.1Mn0.1O2(NCM811)cathodes.Such a rationally designed electrolyte demonstrates excellent flame retardancy,high oxidation stability(5.1 V vs.Li+/Li),and enhanced low-temperature ionic conductivity.As a result,this electrolyte substantially enhances the high-voltage cycle stability(-4.8 V),rate capability(-50 C)and low-temperature cycle performance(-20℃)of Li||NCM811 cells,which retain 80.0%of the initial capacity over 600 cycles at 4.7 V.This research offers a promising strategy to design ideal electrolytes for highperformance Li metal batteries. 展开更多
关键词 Li metal batteries Electrolytes Fluorinated amide Solvation structures Solid electrolyte interphases
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Three-component synthesis of β-acyloxyl alkenyl amides for carboxylic acid/amino acid activation toward peptide and carboxylic acid derivatives synthesis 认领 引用
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作者 Dong-Fang Jiang Fei Zeng +1 位作者 Rong-Nan Yi Wei-Min He 《Chinese Chemical Letters》 SCIE CAS CSCD 2026年第7期1-2,共2页
The formation of peptide bonds is a crucial step in peptide synthesis and their long-term application across diverse fields.Therefore,identifying effective coupling reagents to activate carboxylic and amino acids rema... The formation of peptide bonds is a crucial step in peptide synthesis and their long-term application across diverse fields.Therefore,identifying effective coupling reagents to activate carboxylic and amino acids remains a central objective in peptide chemistry[1].Significant efforts have led to the discovery of numerous coupling agents,including both single-component and combined reagent systems.However,challenges such as high cost,limited commercial availability,un-desired racemization/epimerization,and potential safety hazards continue to hinder ideal peptide synthesis[2]. 展开更多
关键词 peptide synthesis amino acid activation formation peptide bonds activate carboxylic amino acids coupling agentsincluding acyloxyl alkenyl amides carboxylic acid activation coupling reagents
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Deprotection of N-Acyl Indole-Type Amides Based on Si-O Bond Cleavage 认领 引用
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作者 Yang Pengfei Ma Yuting +2 位作者 Xu Wanxin Sun Yumeng Yang Hailing 《有机化学》 SCIE CAS CSCD 北大核心 2026年第5期2112-2120,共9页
The protecting group strategy represents a pivotal approach in organic synthesis,in which the deprotection of amides has garnered considerable attention.However,due to the high stability of the amide bond,harsh condit... The protecting group strategy represents a pivotal approach in organic synthesis,in which the deprotection of amides has garnered considerable attention.However,due to the high stability of the amide bond,harsh conditions are often required for the deprotection of amides.A method for deprotection of amides under mild conditions has been developed,namely the silane-promoted deprotection of N-acyl indole type amides.The Si—O bond of silane undergoes cleavage,generating a nucleophile in situ that attacks the amide bond,thereby successfully achieving the deprotection of amides.The mild conditions,broad substrate scope,operational simplicity,high yields,and the use of inexpensive and readily available reagents,make this protocol a green and practical strategy for deprotection of amides. 展开更多
关键词 N-acyl indole-type amide Si—O bond cleavage deprotection green synthesis
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Advances in biosynthesis of chiral amide herbicides and the key enzymes:dimethenamid-P and S-metolachlor as case studies 认领 引用 被引量：2
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作者 Feng Cheng Yi-Ling Zhou +3 位作者 Dan-Chen Yang Ding-Yi Zhao Ya-Ping Xue Yu-Guo Zheng 《Bioresources and Bioprocessing》 SCIE EI CSCD 2025年第1期241-258,共18页
Chiral amide herbicides represent a significant class of agrochemicals,widely used for effective weed control.Promi-nent examples include S-metolachlor and dimethenamid-P,both of which share the intermediate(S)-1-meth... Chiral amide herbicides represent a significant class of agrochemicals,widely used for effective weed control.Promi-nent examples include S-metolachlor and dimethenamid-P,both of which share the intermediate(S)-1-methoxy-2-propylamine,a key structural component in their synthesis.Developing green and sustainable methods for producing this intermediate is crucial for enhancing the environmental and economic feasibility of herbicide manufacturing.Biosynthesis,with its advantages in sustainability and efficiency,has emerged as a pivotal approach in pesticide production.This review explores the classification and current development status of chiral amide herbicides,including their varieties and applications in the agricultural market.It outlines the synthesis pathways for S-metolachlor and dimethenamid-P,covering both chemical and biosynthetic routes.The review also highlights the functional properties of the key enzymes involved in the biosynthesis of(S)-1-methoxy-2-propylamine,focusing on the potential for enzyme engineering and creation to optimize these pathways.The challenges and future development directions for amide herbicides are discussed,with an emphasis on overcoming synthetic and ecological barriers. 展开更多
关键词 Chiral amide herbicides Biosynthesis S-metochlor Dimethenamid-P (S)-1-methoxy-2-propylamine
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Asymmetric synthesis of chiral N-substituted amino amides and esters with two chiral centers by imine reductase-catalyzed dynamic kinetic resolution via reductive amination 认领 引用 被引量：1
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作者 Zefei Xu Jinhui Feng +5 位作者 Xiangtao Liu Qian Li Weidong Liu Peiyuan Yao Qiaqing Wu Dunming Zhu 《Chinese Journal of Catalysis》 SCIE EI CAS CSCD 2025年第10期144-152,共9页
Chiral N-substituted amino amides and esters are ubiquitous scaffolds in pesticides and pharmaceutical chemicals,but their asymmetric synthesis remains challenging especially for those with multiple chiral centers.In ... Chiral N-substituted amino amides and esters are ubiquitous scaffolds in pesticides and pharmaceutical chemicals,but their asymmetric synthesis remains challenging especially for those with multiple chiral centers.In this study,IR104 from Streptomyces aureocirculatus was identified from 157 wild-type imine reductases for the synthesis of(S)-2-((R)-2-oxo-4-propylpyrrolidin-1-yl)butanamide(antiepileptic drug Brivaracetam)via dynamic kinetic resolution reductive amination from ethyl 3-formylhexanoate and(S)-2-aminobutylamide with high diastereoselectivity.To further improve the catalytic efficiency of IR104,its mutant D191E/L195I/E253S/M258A(M3)was identified by saturation mutagenesis and iterative combinatorial mutagenesis,which exhibited a 102-fold increase in the catalytic efficiency relative to that of wild-type enzyme and high diastereoselectivity(98:2 d.r.).Crystal structural analysis and molecular dynamics simulations provided some insights into the molecular basis for the improved activity of the mutant enzyme.The imine reductase identified in this study could accept chiral amino amides/esters as amino donors for the dynamic kinetic resolution reductive amination of racemicα-substituted aldehydo-esters,expanding the substrate scope of imine reductases in the dynamic kinetic resolution-reductive amination.Finally,IR104-M3 was successfully used for the preparation of Brivaracetam at gram scale.Using this mutant,various N-substituted amino amides/esters with two chiral centers were also synthesized with up to 99:1 d.r.and 96%yields and subsequently converted intoγ-andδ-lactams,providing an efficient protocol for the synthesis of these important compounds via enzymatic dynamic kinetic resolution-reductive amination from simple building blocks. 展开更多
关键词 Imine reductase Dynamic kinetic resolution-reductive amination Directed evolution N-substituted amino amide N-substituted amino ester
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Sustainable carbonylative transformation of alkyl iodides to amides via crosslinking of EDA and XAT 认领 引用 被引量：1
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作者 Hefei Yang Le-Cheng Wang Xiao-Feng Wu 《Chinese Chemical Letters》 SCIE CAS CSCD 2025年第9期318-322,共5页
The amide moiety plays an important role as a powerful bioactive backbone,and as the synthetic chemistry community moves toward more sp3-rich scaffolds,alkyl halides have become the feedstock of choice for obtainin... The amide moiety plays an important role as a powerful bioactive backbone,and as the synthetic chemistry community moves toward more sp3-rich scaffolds,alkyl halides have become the feedstock of choice for obtaining carbonylation products.With the development of photoredox catalysis,several aminocarbonylation systems for alkyl halides were developed which usually require transition metal catalysis.Considering the demands for green sustainable chemical synthesis,here we report a metal-free,exogenous catalyst-free aminocarbonylation reaction of alkyl iodides under atmospheric pressure of carbon monoxide.Through a combination of EDA and XAT strategies,the reaction occurs efficiently under only light irradiation at room temperature. 展开更多
关键词 Carbonylation Amide Metal-free Phtotchemistry Radical
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I2/t-Butylhydroperoxide Mediated Oxidative Coupling of Allylbenzenes with Dialkylformamides to Accessα,β-Unsaturated Amides 认领 引用
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作者 Su Renhua Xiao Duoduo +2 位作者 Zhou Peng Long Yifu Liu Weibing 《有机化学》 SCIE CAS CSCD 北大核心 2025年第12期4463-4467,共5页
A facile one-pot strategy for the synthesis ofα,β-unsaturated amides via an I2-butylhydroperoxide(TBHP)-mediated oxidative system has been reported.The methodology achieves efficient construction of a series ofα... A facile one-pot strategy for the synthesis ofα,β-unsaturated amides via an I2-butylhydroperoxide(TBHP)-mediated oxidative system has been reported.The methodology achieves efficient construction of a series ofα,β-unsaturated amides through oxidative coupling of allylbenzenes with N,N-dialkylformamides under mild conditions.Notably,N,N-dialkylformamides serve as both solvents and reactants in this protocol,significantly enhancing the atom economy of transformation. 展开更多
关键词 I2-butylhydroperoxide allylbenzene N,N-dialkylformamide α,β-unsaturated amide
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Oscillatory flow reactor facilitates fast photochemical Wolff rearrangement toward synthesis ofα-substituted amides in flow 认领 引用
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作者 Huashan Huang Jingze Chen +3 位作者 Luyun Zhang Hong Yan Siqi Li Fen-Er Chen 《Chinese Chemical Letters》 SCIE CAS CSCD 2025年第2期361-365,共5页
A visible light-promoted fast photochemical Wolff rearrangement was developed toward synthesis ofα-substituted amides in continuous flow with the use of a photochemical oscillatory flow reactor(POFR).The control expe... A visible light-promoted fast photochemical Wolff rearrangement was developed toward synthesis ofα-substituted amides in continuous flow with the use of a photochemical oscillatory flow reactor(POFR).The control experiment indicates that a fast process of the Wolff rearrangement(<40 s)is involved.Notably,this protocol does not require excess use of any reactants,and the resultingα-substituted amides could be isolated by recrystallization in good to excellent yields. 展开更多
关键词 Flow photochemistry Oscillatory flow reactor Wolff rearrangement Ketene α-Substituted amides
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New amide alkaloids from Piper longum fruits 认领 引用 被引量：2
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作者 Jun YANG Yao SU +5 位作者 Ji-Feng LUO Wei GU Hong-Mei NIU Yan LI Yue-Hu WANG Chun-Lin LONG 《Natural Products and Bioprospecting》 2013年第6期277-281,共5页
Three new amide alkaloids piperlongumamides A-C(1-3),together with 12 known ones(4-15),were isolated from the fruits of Piper longum.The structures of the new isolates were determined using spectroscopic data analyses... Three new amide alkaloids piperlongumamides A-C(1-3),together with 12 known ones(4-15),were isolated from the fruits of Piper longum.The structures of the new isolates were determined using spectroscopic data analyses.Cytotoxic activity of these amides against HL-60(human leukemia),A-549(human lung cancer),MCF-7(human breast cancer),SMMC-7721(human liver cancer)and SW480(human rectal cancer)cell lines were evaluated.Piperchabamide B(11)exhibited weak inhibitory activity against HL-60(IC50=21.32μM),A-549(IC50=23.82μM)and MCF-7(IC50=16.58μM)cell lines. 展开更多
关键词 Piperaceae Piper longum amide alkaloids piperlongumamides piperchabamide B cytotoxicity
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Carbonylative five-component synthesis of amides and esters withα-quaternary carbon center 认领 引用
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作者 Zhi-Peng Bao Hefei Yang +2 位作者 Ru-Han A Yuanrui Wang Xiao-Feng Wu 《Chinese Chemical Letters》 SCIE CAS CSCD 2025年第11期301-307,共7页
Carboxylic acid derivatives withα-quaternary carbon center are one of the most ubiquitous moieties in synthetic and medicinal chemistry.Hence,novel and efficient synthetic methods towards carboxylic acid derivatives ... Carboxylic acid derivatives withα-quaternary carbon center are one of the most ubiquitous moieties in synthetic and medicinal chemistry.Hence,novel and efficient synthetic methods towards carboxylic acid derivatives withα-quaternary carbon remain in high demand.However,most of the precursors of these complex compounds are not easy to prepare.Reported herein is a carbonylative five-component synthesis of amides and esters withα-quaternary carbon center enabled by palladium catalysis from abundant acrylonitrile,carbon monoxide,fluoroalkyl halides,and nucleophiles.Diverse amides and esters withα-quaternary carbon which contain difluoromethyl or perfluoroalkyl moiety were prepared in good to excellent yields,providing an efficient synthetic platform for sequential transformations. 展开更多
关键词 Carbonylation Palladium catalyst Amide Alkene Multi component reaction
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Copper-catalyzed amide bond formation from formamides and carboxylic acids 认领 引用 被引量：1
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作者 Hong-Qiang Liu Jun Liu +2 位作者 Yang-Hui Zhang Chang-Dong Shao Jing-Xun Yu 《Chinese Chemical Letters》 SCIE CAS CSCD 2015年第1期11-14,共4页
A highly efficient copper-catalyzed approach to form amide bonds from formamides and carboxylic acids was developed. This protocol shows broad substrate scopes and high yields in the presence of 1 mol% catalyst and 4.... A highly efficient copper-catalyzed approach to form amide bonds from formamides and carboxylic acids was developed. This protocol shows broad substrate scopes and high yields in the presence of 1 mol% catalyst and 4.0 equiv, formamides. 展开更多
关键词 Amides Formamides Carboxylic acids Copper Catalysis
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Amide naphthotubes:Biomimetic macrocycles for selective molecular recognition 认领 引用 被引量：4
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作者 Cheng-Da Zhao Huan Yao +3 位作者 Shi-Yao Li Fangfang Du Li-Li Wang Liu-Pan Yang 《Chinese Chemical Letters》 SCIE CAS CSCD 2024年第4期124-131,共8页
Selective molecular recognition in water is routine for bioreceptors,but remains challenging for synthetic hosts.This is principally because noncovalent interactions are usually less efficient in aqueous environments.... Selective molecular recognition in water is routine for bioreceptors,but remains challenging for synthetic hosts.This is principally because noncovalent interactions are usually less efficient in aqueous environments.By mimicking the cavity feature of bioreceptors,Prof.Wei Jiang proposed and clarified the concept of“endo-functionalized cavity”.Through situating polar binding sites into a deep hydrophobic cavity,we designed and synthesized several macrocyclic hosts,among which amide naphthotubes are the most representative.The hosts can selectively recognize various polar molecules including organic micropollutants,drug molecules,and chiral molecules in water by employing the hydrophobic effect and shielded hydrogen bonding.In addition,these biomimetic hosts have been applied in spectroscopic analysis,adsorptive separation and self-assembly.In this review,we provide an overview of recent advances on amide naphthotubes with special emphasis on the efforts of Jiang's group.We are convinced that these biomimetic macrocycles will make further contributions to supramolecular chemistry and beyond. 展开更多
关键词 Molecular recognition Supramolecular chemistry Amide naphthotube Endo-functionalized cavity Biomimetic macrocycle
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Synthesis and Anti-tumor Activity of Novel Amide Derivatives of Ursolic Acid 认领 引用 被引量：9
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作者 LIU Dan MENG Yan-qiu +1 位作者 ZHAO Juan CHEN Li-gong 《Chemical Research in Chinese Universities》 SCIE CAS 2008年第1期42-46,共5页
Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects ... Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3 hydroxyl group show better activities than those with an unsubstituted hydroxyl group. 展开更多
关键词 Ursolic acid Amide derivatives Anti-tumor activity
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Measurement and Correlation for Solubility of (S)-(+)-2,2-Dimethylcyclopropane Carbox Amide in Different Solvents 认领 引用 被引量：7
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作者 石晓华 周彩荣 +1 位作者 高玉国 陈新志 《Chinese Journal of Chemical Engineering》 SCIE EI CAS 2006年第4期547-550,共4页
（S）-（＋）-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of dehydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial... （S）-（＋）-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of dehydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of （S）-（＋）-2,2-dimethylcyclopropane carbox amide in toluene, dichloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured using the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation.The calculated values were good in agreement with the experimental values. 展开更多
关键词 solid-liquid equilibrium solubility （S）-（＋）-2 2-dimethylcyclopropane carbox amide
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Synthesis and biological evaluation of 12-benzyl matrinic amide derivatives as a novel family of anti-HCV agents 认领 引用 被引量：5
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作者 Sheng Tang Zong-Gen Peng +5 位作者 Xin Zhang Xin-Yue Cheng Wen-Jing Li Jian-Dong Jiang Ying-Hong Li Dan-Qing Song 《Chinese Chemical Letters》 SCIE CAS CSCD 2016年第7期1052-1057,共6页
A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine（1）and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suita... A new series of 12-benzyl matrinic amide/ethanamide derivatives were synthesized from matrinine（1）and evaluated for their anti-HCV activity,taking compound 2 as the lead.SAR revealed that the introduction of a suitable substituent at the N’-end of matrinic amide might greatly enhance the potency.Among them,matrinic acid 17 and N’-substituted matrinic amides 18a-d exhibited promising potency with low micromolar EC50 values ranging from 1.03μmol/L to 7.54 μmol/L,and better therapeutic window with SI from 66 to 132.Moreover,compound 17 displayed an excellent PK and safety profile in vivo,demonstrating good drug-like characteristics.Thus,it has been selected for further investigation,with an advantage of decreased chances of inducing drug-resistance mutations. 展开更多
关键词 Matrinic acid Matrinic amide Hepatitis C virus Structure–activity relationship
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The Anticancer Activities Phenolic Amides from the Stem of Lycium barbarum 认领 引用 被引量：7
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作者 Pei-Feng Zhu Zhi Dai +6 位作者 Bei Wang Xin Wei Hao-Fei Yu Zi-Ru Yan Xu-Dong Zhao Ya-Ping Liu Xiao-Dong Luo 《Natural Products and Bioprospecting》 2017年第6期421-431,共11页
Four new phenolic amides,4-O-methylgrossamide(1),(E)-2-(4,5-dihydroxy-2-{3-[(4-hydrox-yphenethyl)amino]-3-oxopropyl}-phenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenethyl)acryl-amide(2),(Z)-lyciumamide C(3),(Z)-... Four new phenolic amides,4-O-methylgrossamide(1),(E)-2-(4,5-dihydroxy-2-{3-[(4-hydrox-yphenethyl)amino]-3-oxopropyl}-phenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenethyl)acryl-amide(2),(Z)-lyciumamide C(3),(Z)-thoreliamide B(4),together with thirteen known phenolic amides were identified from the stem of Lycium barbarum.The structures of the new compounds were determined by spectroscopic methods.All compounds were evaluated for their anti-cancer activities against human glioma stem cell lines. 展开更多
关键词 Lycium barbarum Phenolic amides Anticancer activities Glioma stem cell
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