专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
专利号:US-2008176857-A1 优先权日:2005-03-25 标题 :4-Piperazinnylthieno[2,3-d]Pyrimidine Compounds as Platelet Aggregation Inhibitors 发明人:ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; TENBRINK RUTH ELIZABETH 权利人:ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; TENBRINK RUTH ELIZABETH 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: n n n n n n n n n n wherein A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , X 4 , X 6 , R 2 , R 4 , R 5 , and R 6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2008280877-A1 优先权日:2007-05-10 标 题:Azetidines 发明人:DACK KEVIN NEIL; SKERRATT SARAH ELIZABETH; YEAP SIEW KUEN 权利人:PFIZER 摘要:The invention relates to EP2 antagonist azetidines of formula (I) n n n n n n n n n n wherein Ar, R 1 , X, and Z are as defined herein, to their use in medicine, particularly in the treatment of endometriosis and/or uterine fibroids, to intermediates useful in their synthesis, and to compositions containing them.
专利号:US-9115102-B2 优先权日:2009-09-17 标题 :N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors 发明人:CHAMBON SANDRINE; CLARY LAURENCE; SCHUPPLI MARLENE 权利人:CHAMBON SANDRINE; CLARY LAURENCE; SCHUPPLI MARLENE; GALDERMA RES & DEV 摘要:The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.
参考标题:Merging Gold Catalysis, Organocatalytic Oxidation, And Lewis Acid Catalysis For Chemodivergent Synthesis Of Functionalized Oxazoles From N-Propargylamides 作者:Shaoyu Mai,Changqing Rao,Ming Chen,Jihu Su,Jiangfeng Du,Qiuling Song 摘要:Novel Catalytic Systems Consisting Of Cationic Gold Complexes, N-Hydroxyphthalimide (Nhpi), And Transition-Metal-Based Lewis Acids Have Been Developed For The One-Pot Synthesis Of Functionalized Oxazoles From N-Propargylamides With Excellent Functional Group Tolerance. These Transformations Demonstrated The Excellent Compatibility Of Homogeneous Gold Catalysis With Organocatalytic Oxidative Carbon-Nitrogen