4-(4-氯苯基)-4-氧代丁酸甲酯 反应生成3-(4-氯苯甲酰)丙酸 参考文献:The Use Of Organocadmium Reagents For The Preparation Of Substituted β-Aroylpropionic Acids 标题:The Use Of Organocadmium Reagents For The Preparation Of Substituted β-Aroylpropionic Acids 摘要: Doi:10.1021/jo01150A010
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6132953-A 优先权日:1996-07-02 标 题 :Combinatorial synthesis on soluble polyvalent supports having a discrete architecture 发明人:CHAPMAN KEVIN T; HUTCHINS STEVEN M; KIM RONALD M; MANNA MAHUA 权利人:MERCK & CO INC 摘要:The present invention is directed to the use of a soluble polyvalent support for the preparation of combinatorial libraries of compounds. The resultant combinatorial libraries are useful in screening for biologically active moieties in the drug discovery process or in developing compounds with desired physical and chemical properties.
专利号:US-11884628-B2 优先权日:2019-05-16 标题 :Method for synthesizing lactam derivatives without use of catalyst 发明人:YANG SONG; LI HU; WU HONGGUO 权利人:UNIV GUIZHOU 摘要:Disclosed is a simple synthesis method of lactam derivatives, comprising: with formamide functioning as both an amine source and a hydrogen source (hydrolyzed to produce formic acid), carrying out a cycloamination reaction on a raw material keto acid in the absence of a solvent or a catalyst to simply synthesize a lactam derivative. Compared with previous reports, the present disclosure has the following advantages: the time required for the reaction is greatly shortened, the selectivity is remarkably improved, a conversion rate of a keto acid derivative is greater than 99%, and the yield of the lactam derivative can reach 70% to 94%.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:EA-002100-B1 优先权日:1996-12-23 标题:CYCLOALCYL COMPOUNDS, LACTAMS, LACTONES AND RELATED COMPOUNDS CONTAINING THEIR PHARMACEUTICAL COMPOSITIONS AND METHODS OF INHIBITING THE SURVIVAL AND / OR SYNTHESIS OF β-AMYLOUS PEPTIDE SOFTWARE AGREED SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE, SOFTWARE AND SOFTWORK
参考标题:A Facile Direct Route To N ‐(Un)Substituted Lactams By Cycloamination Of Oxocarboxylic Acids Without External Hydrogen 作者:Hu Li,Hongguo Wu,Heng Zhang,Yaqiong Su,Song Yang,Emiel J. M. Hensen |发布日期:2019.8.22 摘要:Lactams Are Privileged In Bioactive Natural Products And Pharmaceutical Agents And Widely Featured In Functional Materials. This Study Presents A Novel Versatile Approach To The Direct Synthesis Of Lactams From Oxocarboxylic Acids Without Catalyst Or External Hydrogen. The Method Involves The In Situ Release Of Formic Acid From Formamides Induced By Water To Facilitate Efficient Cycloamination. Water