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1. 发明公开

KR1020000005286A 치료용 아미드의 입체선택성 제조를 위한 효소적 공정 无效
标题翻译：用于治疗药物的立体选择性制备的酶学方法
公开(公告)号：KR1020000005286A
公开(公告)日：2000-01-25
申请号：KR1019980707994
申请日：1997-04-07
申请人： 신젠타 리미티드
发明人： 크로스비존 , 홀트로버트안토니 , 피탐존데비드
IPC分类号： C12P13/02
CPC分类号： C12P13/00 , C07C255/11 , C07C255/14 , C12P7/40 , C12P7/42 , C12P13/02 , C12P41/004 , C12P41/005
摘要： PURPOSE: An enzymatic process for stereo selective preparation of N-aryl or -pyridyl propanamides having a tertiary alcohol stereogenic center is provided. The N-aryl or -pyridyl propanamides are cellular potassium channel opener and are thus useful in the treatment of urinary incontinence, hypertension, asthma, peripheral vascular disease and angina. Also, provided is a process for stereo selective synthesis of enantiomer intermediates useful in the synthesis of such compound. CONSTITUTION: The first process comprises preparing an optically active compound, N-aryl or -pyridyl propanamide of formula I by treating a racemic compound of formula II with a hydrolase and the second process comprises treating a racemic compound, an ester of 3,3,3-trifluro-2-hydroxy-2-methylpropanoic acid of formula V with a hydrolase.
摘要翻译：目的：提供立体选择性制备具有叔醇立体中心的N-芳基或吡啶基丙酰胺的酶促方法。 N-芳基或吡啶基丙酰胺是细胞钾通道开放剂，因此可用于治疗尿失禁，高血压，哮喘，外周血管疾病和心绞痛。此外，提供了用于合成这种化合物的对映异构体中间体的立体选择性合成方法。构成：第一种方法包括通过用水解酶处理式II的外消旋化合物来制备式I的光学活性化合物N-芳基或吡啶基丙酰胺，第二种方法包括处理外消旋化合物，3,3，具有式V的3-三氟-2-羟基-2-甲基丙酸与水解酶。

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