CAS: 720720-96-7; 5-Methyl-4,5,6,7-Tetrahydrothiazolo[5,4-C]Pyridine-2-Carboxylic Acid Hydrochloride

2-溴-5-甲基-4,5,6,7-四氢噻唑[4-C]哌啶置于sodium Dithionite,Lithium Hydroxide Monohydrate,三乙胺体系中,用 乙醇,水,甲苯 作为反应溶剂,化学反应生成 4,5,6,7-四氢-5-甲基-噻唑并[5,4-C]吡啶-2-羧酸盐酸盐
参考文献:一种依度沙班的制备方法
标题:一种依度沙班的制备方法
摘要:本发明涉及对甲苯磺酸依度沙班水合物及其中间体的制备新路线和新方法.包括:制备了具有高反应活性的化合物109A4X;采用新的合成方法制备化合物109C6X;制备了新的化合物109E8‑01,109E9X,109T7‑01;并用上述中间体制备得到对甲苯磺酸依度沙班水合物.新方法和新路线避免了需要深冷的反应步骤,避免了用危险的单质硫和高风险的正丁基锂,高危险性的叠氮化合物.总之,本发明的方法更利于安全,简便并有效降低成本的工业化规模来制备对甲苯磺酸依度沙班水合物及其关键中间体.

专利信息

专利号:US-2015239909-A1
优先权日:2012-11-23
标 题 :Process for the preparation of (1s,4s,5s)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one
发明人：NAKAMURA YOSHITAKA; MUKESH Kumar Madhra; INAMDAR MURAD ISMAIL
权利人:DAIICHI SANKYO CO LTD
摘要:The present invention relates to an improved and industrially advantageous process for the preparation of (1S, 4S, 5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one represented by the following formula (1) n n n n n n n n n n which is a key intermediate in the synthesis of edoxaban, a compound that exhibits on inhibitory effect on activated blood coagulation factor X (also referred to as activated factor X or FXa), and is useful as a preventive and/or therapeutic drug for thrombotic diseases. The process includes reacting (1S)-cyclohex-3-ene-1-carboxylic acid of formula (II) with a brominating agent selected from the group consisting of N-bromosuccinimide or 1,3-dibromo-5, 5-dimethylhydantoin in the presence of a base selected from calcium oxide or calcium hydroxide in a solvent selected from the group comprising of dicholoromethane, toluene, tetrahydrofuran, ethyl acetate, hexanes, cyclopentyl methyl ether (CPME) or a misture thereof to get (1S, 4S 5S)-4-bromo-6-oxabicyclo[3.2.1]octan-y-one of formula (1)

专利号:US-9809546-B2
优先权日:2016-03-14
标 题 :Process for producing diamine derivative
发明人：LU TZU-CHIANG; CHEN CHIEN-YI; CHENG CHING-SHUEN; MAI CHIN-CHENG
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD; CHUNGWHA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:The present invention provides a low-toxic and high-recovery industrial process for synthesizing an optically active diamine derivative represented by formula (D), the process comprising the steps of: (a) mixing a compound represented by formula (A) and a compound represented by formula (C) in organic solvents and secondary amine; (b) reaction under heating; (c) cooling and adding water to the mixed solution, allowing it to crystallize to obtain the compound represented by formula (D).

专利号:CN-117384186-A
优先权日:2023-10-12
标 题:Synthesis method of intermediate for preparing edoxaban