CAS: 181140-34-1; (R)-2-(Oxiran-2-Ylmethyl)Isoindoline-1,3-Dione

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CAS号57044-25-4 (|R|)-(+)-缩水甘油 | CAS号19667-37-9 2-(3-氯-2-羟基丙基)异... | CAS号51594-55-9 左旋环氧氯丙烷 | CAS号67843-74-7 (S)-(+)-环氧氯丙烷 | CAS号1074-82-4 邻苯二甲酰亚胺钾盐 | CAS号641617-21-2 (R)-1-phthalimi...

2-(3-氯-2-羟基丙基)异吲哚-1,3-二酮置于potassium Carbonate,Amano Ps-Im Lipase From Burkholderia Cepacia体系中,用 四氢呋喃,甲苯 用作溶剂,化学反应 96.0H,反应生成(R)-N-环氧丙基邻苯二甲酰亚胺
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-9884844-B2
优先权日:2012-12-31
标 题:Heterocyclic compounds and methods of use thereof
发明人：FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L
权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

专利号:US-2005215801-A1
优先权日:2002-06-28
标 题 :Process for preparation of optically active 1-substituted amino-2,3-epoxypropanes, intermediates for synthesis thereof and process for preparation of the intermediates
发明人：KITAJIMA KUMI; NAGASHIMA NOBUO
权利人:KITAJIMA KUMI; NAGASHIMA NOBUO
摘要:The present invention provides an industrial process for effectively and advantageously preparing optically active 1-substituted amino-2,3-epoxypropanes useful as intermediates for preparing agricultural chemicals and medical products from optically active 1-substituted amino-2,3-propanediols used as raw materials. The present invention also provides useful intermediates. Specifically, an optically active 1-substituted amino-2,3-propanediol (1) is reacted with an orthoacid ester (2) or thionyl chloride (3) to produce a cyclic optically active compound (4), and then a compound (5) containing a halogen atom is prepared by reaction with a ring-opening reaction agent having an ability to introduce a halogen atom X. Finally, an optical active 1-substituted amino-2,3-epoxypropane is prepared by ring-closure reaction in the presence of a base.

专利号:EP-1553093-A1
优先权日:2002-06-28
标 题 :Process for preparation of optically active 1-substituted amino-2,3-epoxypropanes, intermediates for the synthesis thereof and process for preparation of the intermediates