CAS: 161596-47-0; (S)-2-(Oxiran-2-Ylmethyl)Isoindoline-1,3-Dione

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181140-34-1 5455-98-1 161596-47-0

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2-(3-氯-2-羟基丙基)异吲哚-1,3-二酮置于硫酸,Potassium Carbonate,Amano Ps-Im Lipase From Burkholderia Cepacia体系中,用 甲醇,甲苯 用作溶剂,化学反应 192.0H,反应生成(S)-N-缩水甘油邻苯二甲酰亚胺
参考文献:开发对映体富集的 β-肾上腺素分解剂的新型化学酶途径.关于普萘洛尔,阿普洛尔,吲哚洛尔,卡拉唑洛,莫普洛尔和美托洛尔的案例研究.
标题:开发对映体富集的 β-肾上腺素分解剂的新型化学酶途径.关于普萘洛尔,阿普洛尔,吲哚洛尔,卡拉唑洛,莫普洛尔和美托洛尔的案例研究.
摘要:合成肾上腺素能 β 受体阻滞剂的两种对映异构体的有效化学酶途径是通过鉴定中心手性结构单元来完成的,该结构单元首先使用脂肪酶催化动力学拆分 (Kr,Amano Ps-Im) 作为 5 克的不对称步骤制备-刻度(209 Mm 浓度).随后获得的对映体纯 (R)-氯醇 (>99% Ee) 用于合成一系列模型 (R)-(+)-β-受体阻滞剂(即普萘洛尔,阿普洛尔,吲哚洛尔,卡唑洛尔,莫普洛尔和美托洛尔),其产生的对映体过量在 96-99.9% 范围内.以普萘洛尔为模型的药学相关 (S)-对应物是通过使用乙酸铯和催化量的 18-Crown 对各自的对映体纯 (R)-甲磺酸盐进行乙酰解以优异的对映体纯度 (99% Ee) 合成的-6,然后将形成的(S)-乙酸酯进行酸水解.或者,使用含有来自乳酸杆菌的过表达重组乙醇脱氢酶的冻干大肠杆菌细胞进行前手性酮的不对称还原,即 2-(3-Chloro-2-Ox
Doi:10.1039/d2Ra04302E

专利信息

专利号:US-11891384-B2
优先权日:2017-01-04
标题:Process for the preparation of Rivaroxaban involving novel intermediate
发明人：SATHE DHANANJAY G; DAS ARIJIT; Raikar Sanjay; SURVE YASHWANT S; PANDIT BHUSHAN S
权利人:UNICHEM LAB LTD
摘要:The present invention relates to the novel key intermediate, 4-{4-[(SS)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, m the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.

专利号:WO-2006031179-A1
优先权日:2004-09-13
标 题:Process for preparation of phtalimide
发明人：KRIG ANN-SOFIE; THELIN MATS
权利人:ASTRAZENECA AB; KRIG ANN-SOFIE; THELIN MATS
摘要:The present invention is directed to a novel process for the synthesis of (S) -glycidyl phthalimide and to novel intermediates in the process. The process comprises, reacting a (R) -3 -Chloro-1,2-propanediol and phtalimide salt. Then reacting the product with trimethylorthoacetate and an essentially water free acid. Then reacting the product with acetyl halogenide and do a basic ester hydrolysis.

专利号:WO-2015198259-A1
优先权日:2014-06-26
标 题:Process for the synthesis of rivaroxaban and intermediate for the production thereof
发明人：FERRARI MASSIMO; GHEZZI EMANUELE; GHEZZI MARCELLO
权利人:ERREGIERRE SPA
摘要:A process is described for the production of Rivaroxaban, a compound having the following structural formula: (I) by means of obtaining a novel intermediate of said process.

专利号:RU-2383540-C2
优先权日:2004-01-15
标 题 :Method for synthesis of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide