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1. 发明申请

US20060106221A1 Process for the preparation of thiazolidinedione derivatives 审中-公开
标题翻译：噻唑烷二酮衍生物的制备方法
公开(公告)号：US20060106221A1
公开(公告)日：2006-05-18
申请号：US11326003
申请日：2006-01-05
申请人： Robert Giles , Norman Lewis , John Quick
发明人： Robert Giles , Norman Lewis , John Quick
IPC分类号： A61K31/4439 , C07D417/02
CPC分类号： C07D417/12
摘要： A process for preparing a compound of formula (I): or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein: A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; A2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6, which process comprises catalytically reducing a compound of formula (II): wherein A1, R1, A2 and n are as defined in relation to formula (I), characterised in that the reduction reaction is carried out using a hydrogen pressure above 20 psi; and thereafter if required forming a pharmaceutically acceptable salt and/or a pharmaceutically acceptable solvate of the compound of formula (I).
摘要翻译：制备式（I）化合物或其互变异构体或其药学上可接受的盐或其药学上可接受的溶剂合物的方法，其中：A 1表示取代或未取代的芳族杂环基 ; R 1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; 代表一个总共有五个取代基的苯环; 并且n表示2至6的整数，该方法包括催化还原式（II）的化合物：其中A 1，R 2， SUP> 2和n如关于式（I）所定义，其特征在于还原反应使用高于20psi的氢气压力进行; 然后如果需要，形成式（I）化合物的药学上可接受的盐和/或药学上可接受的溶剂化物。

2. 发明申请

US20070066662A1 PROCESS FOR THE PREPARATION OF THIAZOLIDINEDIONE DERIVATIVES 失效
标题翻译：制备噻唑啉衍生物的方法
公开(公告)号：US20070066662A1
公开(公告)日：2007-03-22
申请号：US11550506
申请日：2006-10-18
申请人： Robert Giles , Norman Lewis , John Quick
发明人： Robert Giles , Norman Lewis , John Quick
IPC分类号： A61K31/4439 , C07D417/02
CPC分类号： C07D417/12
摘要： A process for preparing a compound of formula (I): or a tautomeric form thereof or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein: A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; A2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6, which process comprises catalytically reducing a compound of formula (II): wherein A1, R1, A2 and n are as defined in relation to formula (I), characterised in that the reduction reaction is carried out using a hydrogen pressure above 20 psi; and thereafter if required forming a pharmaceutically acceptable salt and/or a pharmaceutically acceptable solvate of the compound of formula (I).
摘要翻译：制备式（I）化合物或其互变异构体或其药学上可接受的盐或其药学上可接受的溶剂合物的方法，其中：A 1表示取代或未取代的芳族杂环基 ; R 1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; 代表一个总共有五个取代基的苯环; 并且n表示2至6的整数，该方法包括催化还原式（II）的化合物：其中A 1，R 2， SUP> 2和n如关于式（I）所定义，其特征在于还原反应使用高于20psi的氢气压力进行; 然后如果需要，形成式（I）化合物的药学上可接受的盐和/或药学上可接受的溶剂化物。

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