CAS: 1513-45-7; 4-(Trifluoromethoxy)Benzenesulfonamide

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1129-26-6 874781-09-6 909527-60-2

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CAS号94108-56-2 4-(三氟甲氧基)苯磺酰氯

4-(三氟甲氧基)苯磺酰氯置于ammonium Hydroxide体系中,用 1,4-二氧六环 用作溶剂,化学反应 1.0H,以83%的收率获得4-三氟甲氧基苯磺酰胺
参考文献:合理设计的多药理学:α-螺旋模拟物作为癌蛋白 Mcl-1 和 Hdm2 的双重抑制剂.
标题:合理设计的多药理学:α-螺旋模拟物作为癌蛋白 Mcl-1 和 Hdm2 的双重抑制剂.
摘要:蛋白质-蛋白质相互作用(ppi),其中许多以 α 螺旋识别域为主,在许多重要的细胞过程中发挥着关键作用,这些相互作用的失调可能会导致有害影响.例如,涉及 Bcl-2 蛋白家族的异常 Ppi 可导致多种疾病,包括癌症,神经退行性疾病和糖尿病.Bcl-2 促生命蛋白(例如 Mcl-1)与促死亡蛋白(例如 Bim)之间的相互作用调节细胞凋亡的内在途径.P53 是一种肿瘤抑制蛋白,在细胞凋亡中也发挥着关键作用,并受到其 E3 泛素连接酶 Hdm2 的负向调节.Mcl-1 和 Hdm2 在许多癌症中均上调,有趣的是,这两种蛋白质途径之间存在串扰.最近,观测到 Mcl-1 和 Hdm2 抑制剂之间的协同作用.为了开发新的抗癌药物,我们在此描述了一种多重药理学方法,通过使用三种密集功能化的异恶唑,吡唑和噻唑作为其伴侣蛋白关键 α 螺旋结构域的模拟物,来双重抑制 Mcl-1 和 Hdm2.
Doi:10.1002/cmdc.202000278

专利信息

专利号:US-11479577-B2
优先权日:2016-05-18
标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
发明人：WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS
权利人:NZP UK LTD
摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

专利号:US-10766921-B2
优先权日:2016-05-18
标 题 :Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes
发明人：WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY
权利人:NZP UK LTD
摘要:The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

专利号:US-2019284227-A1
优先权日:2016-05-18
标题:Intermediates for the Synthesis of Bile Acid Derivatives, in Particular of Obeticholic Acid

专利号:WO-2017199033-A1
优先权日:2016-05-18
标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid

专利号:US-10450282-B2
优先权日:2015-08-06
标题:Stereospecific process for 3-heterocyclylcycloaliphatic-1,2-diols
发明人：OHLMEYER MICHAEL; ZAWARE NILESH; KASTRINSKY DAVID
权利人:ICAHN SCHOOL MED MOUNT SINAI
摘要:A process for the stereoselective synthesis of chiral 3-heterocyclyl-1,2-dihydroxy cyclohexanes is disclosed. The process involves reacting a tricyclic nitrogenous heterocycle with an allyl carbonate in the presence of a chiral palladium catalyst followed by oxidation of the olefinic bond to provide 3-heterocyclyl-1,2-dihydroxy cyclohexanes, cyclopentanes and corresponding alicyclic heterocycles. Also disclosed are methods for converting the heterocyclyl-1,2-dihydroxy cyclohexanes to 2-amino-6-(heteroaryl)cyclohexanols (and related cyclic compounds).

专利号:US-10968250-B2
优先权日:2016-05-18
标 题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid