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1. 发明申请

US20060276659A1 Process for preparation of perindopril and salts thereof 有权
标题翻译：培哚普利及其盐的制备方法
公开(公告)号：US20060276659A1
公开(公告)日：2006-12-07
申请号：US10547243
申请日：2003-02-28
申请人： Debashish Datta , Girij Singh , Himanshu Godbole , Rajinder Siyan
发明人： Debashish Datta , Girij Singh , Himanshu Godbole , Rajinder Siyan
IPC分类号： C07D209/42
CPC分类号： C07D209/42 , C07C227/32 , C07C227/34 , C07C229/12
摘要： A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe convenient and cost-effective. The process involves reaction of compound of formula (I), wherein X is chlorine or bromine with compound of formula (VII) wherein A signifies that the six-membered ring of the bicyclic system is either saturated or unsaturated to give compound of formula (VIII), wherein A is as defined above, followed by catalytic hydrogenation of the compound of formula (VIII) thus obtained to give the perindopril of formula (II). The above process for the manufacture of perindopril would specifically avoid the use of harmful chemicals like phosgene or costly coupling agents like dicyclohexylcarbodiimide and 1-hydroxybenxotriazole usually used for such manufacture. The process would also not require any intervention of a catalyst and does not require any alkaline or acidic reaction conditions. Importantly, the process provides for manufacture of perindopril with high stereoselectively giving perindopril (II) having (S)-configuration in all the five chiral centres of the molecule, conforming to pharmacoepeial specifications. The invention also relates to a method for preparation of the compound of formula (I) and also to a method for preparation of N-[(S)-1-carbethoxybutyl]-(S)-alanine of formula (III) used in the process.
摘要翻译：制备式（II）的培哚普利及其盐的方法，其简单，安全的方便和成本有效。该方法包括式（I）化合物，其中X是氯或溴与式（Ⅶ）化合物反应，其中A表示双环系统的六元环是饱和或不饱和的，得到式（Ⅷ）化合物），其中A如上所定义，然后将由此获得的式（VIII）化合物进行催化氢化，得到式（II）的培哚普利。上述制造培哚普利的方法将特别避免使用通常用于制造的有害化学物质如光气或昂贵的偶联剂如二环己基碳二亚胺和1-羟基苯并三唑。该方法也不需要任何催化剂的干预，并且不需要任何碱性或酸性反应条件。重要的是，该方法提供了高度立体选择性地给予符合药代动力学规范的在分子的所有五个手性中心具有（S） - 构型的培哚普利（II）的培哚普利的培哚普利。本发明还涉及制备式（I）化合物的方法，还涉及制备式（III）化合物的N - [（S）-1-甲氧基丁基] - （S） - 丙氨酸的方法，处理。

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