1,3-二氯苯置于磺酰氯,硫酸体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 2.5H,以62%的收率获得2,4-二氯苯磺酰氯 参考文献:Sulfonyl Chloride As A Disposable Electron Withdrawing Substituent In Halex Fluorinations 标题:Sulfonyl Chloride As A Disposable Electron Withdrawing Substituent In Halex Fluorinations 摘要:Syntheses Of 1,3-Difluorobenzene And 2,6-Difluorotoluene Are Described Via Chlorosulfonation,Catalytic Halex-Fluorination,And Desulfination Of 1,3-Dichlorobenzene And 2,6-Dichlorotoluene. (C) 2000 Elsevier Science S.A. All Rights Reserved. Doi:10.1016/s0022-1139(99)00195-5
专利号:US-2012053350-A1 优先权日:2009-04-30 标题 :Preparation of alkyl esters of n-protected oxo-azacycloalkylcarboxylic acids 发明人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 权利人:MANGION IAN; HUFFMAN MARK A; RUCK REBECCA T; LYNCH JOSEPH; CHUNG JOHN Y L; MARCUNE BENJAMIN 摘要:A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein P G1 is an amine protective group; k is 0, 1, or 2; and R U , R 1 , R 2 , and R 3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (R U ) 3 S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
专利号:US-9604985-B2 优先权日:2013-06-10 标 题 :Process for the preparation of chiral tert-butyl 4-((1R,2S,5R)-6(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carb derivatives and (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide 发明人:MILLER STEVEN P; LIMANTO JOHN; ZHONG YONG-LI; YASUDA NOBUYOSHI; LIU ZHIJIAN 权利人:MERCK SHARP & DOHME 摘要:A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R 4 —SO 2 W (II-Su) in the presence of tertiary amine base, wherein P G1 and P G2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
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:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC
专利号:US-2020149034-A1 优先权日:2017-03-17 标题:Methods and Compositions for Synthesis of Encoded Libraries