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公开(公告)号:US20130190487A1
公开(公告)日:2013-07-25
申请号:US12524346
申请日:2008-01-24
申请人: Anton Stimac , Barbara Mohar , Michel Stephan , Mojca Bevc , Rok Zupet , Andrej Gartner , Vesna Kroselj , Matej Smrkolj , Davor Kidemet , Gregor Sedmak , PRIMOZ BENKIC , ALEN KLJAJIC , MIHA PLEVNIK
发明人: Anton Stimac , Barbara Mohar , Michel Stephan , Mojca Bevc , Rok Zupet , Andrej Gartner , Vesna Kroselj , Matej Smrkolj , Davor Kidemet , Gregor Sedmak , PRIMOZ BENKIC , ALEN KLJAJIC , MIHA PLEVNIK
IPC分类号: C07D205/08
CPC分类号: C07D205/08 , C07D403/06
摘要: The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields and purity in a fast and cost efficient manner. The present invention relates to a novel crystalline form of ezetimibe as well.
摘要翻译: 本发明涉及依泽替米贝的制备方法,特别涉及其合成的新型中间体以及制备这种中间体的改进方法。 所述中间体可以快速且成本有效的方式以高产率和纯度获得。 本发明还涉及一种新型的依泽替米贝的结晶形式。
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公开(公告)号:US20060040921A1
公开(公告)日:2006-02-23
申请号:US10541604
申请日:2004-01-16
申请人: Roman Lenarsic , Rok Zupet , Milena Benedik , Barbara Mohar , Anton Stimac
发明人: Roman Lenarsic , Rok Zupet , Milena Benedik , Barbara Mohar , Anton Stimac
IPC分类号: A61K31/551 , C07D498/02
CPC分类号: C07D495/04 , C07D243/14
摘要: The invention provides an improved process for preparing Olanzapine as well as intermediates therefor.
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公开(公告)号:US06252091B1
公开(公告)日:2001-06-26
申请号:US09668101
申请日:2000-09-22
IPC分类号: C07D30930
CPC分类号: C07D309/30 , Y02P20/55
摘要: A process for the preparation of compounds of formula (I) wherein R is a C1 to C12 alkyl group and R1 is a protecting group or H which process comprises (a) converting the diol lactone of formula (II) to the protected diol lactone of formula (IIa) wherein R1 is a protecting group (b) acylating the protected diol lactone (IIa) to give compound (I) wherein R1 is a protecting group, (c) optionally removing the protecting group R1 to give compound (I) wherein R1 is H; and wherein steps (a) and/or (b) are carried out in the presence of N-methylimidazole.
摘要翻译: 制备式(I)化合物的方法,其中R是C1-C12烷基,R1是保护基或H,其方法包括(a)将式(II)的二醇内酯转化成式(IIa)的被保护的二醇内酯 )其中R1是保护基团(b)酰化保护的二醇内酯(IIa)以得到其中R 1为保护基的化合物(I),(c)任选地除去保护基团R 1,得到其中R 1为H ; 步骤(a)和/或(b)在N-甲基咪唑存在下进行。
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