CAS: 480452-36-6; Tert-Butyl ((1R,2S,5S)-2-(2-((5-Chloropyridin-2-yl)Amino)-2-Oxoacetamido)-5-(Dimethylcarbamoyl)Cyclohexyl)Carbamate

上下游产品

tert-butyl N-[(1R,2S,5S)-2-azido-5-[(dimethylamino)carbonyl]cyclohexyl]carbamate 5-chloro-2-pyridylamine (1S,3S,6R)-N,N-dimethyl-7-oxabicyclo[4.1.0]heptane-3-carboxamide (1S,3R,4R)-3-amino-4-hydroxy-N,N-dimethyl cyclohexanecarboxamideedoxaban [14C]-Edoxaban tosylate 1-[(1S,2R,4S)-2-amino-4-[(dimethylamino)carbonyl]cyclohexyl]-N2-(5-chloro-2-pyridyl)ethanediamideN1-[(1S,2R,4S)-2-amino-4-[(dimethylamino)carbonyl]cyclohexyl]-N2-(5-chloro-2-pyridyl)ethanediamide

3-环己烯-1-甲酸置于ammonium Hydroxide,Sodium Azide,Lithium Hydroxide Monohydrate,Palladium On Activated Charcoal,碘,甲酸铵,三乙胺,Potassium Iodide,Sodium Hydroxide体系中,用 四氢呋喃,乙醇,二氯甲烷,水,N,N-二甲基甲酰胺,丙酮 作为反应溶剂,化学反应 129.0H,反应生成 [(1R,2S,5S)-2-[[2-[(5-氯吡啶-2-基)氨基]-2-氧代乙酰基]氨基]-5-(二甲基氨基羰基)环己基]氨基甲酸叔丁酯
参考文献:甲苯磺酸艾多沙班及其异构体的制备方法
标题:甲苯磺酸艾多沙班及其异构体的制备方法
摘要:本发明公开了一种甲苯磺酸艾多沙班及其异构体的制备方法,以化合物(I)和化合物(II)为起始原料,可用于制备高纯度的甲苯磺酸艾多沙班(1S,2R,4S),甲苯磺酸艾多沙班对映异构体(1R,2S,4R),甲苯磺酸伊多沙班差向异构体(1R,2R,4S)和甲苯磺酸伊多沙班差向异构体(1S,2S,4R)中任意一种物质,为甲苯磺酸艾多沙班原料药及相关制剂的工艺研究和质量控制提供了有效的保障,且该制备方法适合商业化,生产的甲苯磺酸艾多沙班原料药纯度高,具有重大的意义与实用的价值,有利于甲苯磺酸艾多沙班的原料药生产和药品质量控制.

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).