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3. 发明授权

US06175014B1 Process for the preparation of lactam derivatives 失效
标题翻译：制备内酰胺衍生物的方法
公开(公告)号：US06175014B1
公开(公告)日：2001-01-16
申请号：US08137228
申请日：1993-10-18
申请人： Ian Harold Coates , Alexander William Oxford , Peter Charles North , Thomas Miller , Anthony David Baxter , Kevin Ian Hammond
发明人： Ian Harold Coates , Alexander William Oxford , Peter Charles North , Thomas Miller , Anthony David Baxter , Kevin Ian Hammond
IPC分类号： C07D23361
CPC分类号： C07D471/04 , C07D487/04 , Y02P20/55
摘要： The invention provides a process for the preparation of a compound of general formula (I): wherein Im represents an imidazolyl group of the formula: and R1 represents a hydrogen atom or a group as herein defined including —CO2R5, —COR5, —CONR5R6 or —SO2R5 wherein R5 and R6, which may be the same or different, are as herein defined with the proviso that R5 does not represent a hydrogen atom when R1 represents a group —CO2R5 or —SO2R5; one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6alkyl, C3-7cycloaklyl, C3-6alkenyl, phenyl or phenyl C1-3alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6alkyl group; and n represents 2 or 3; which comprises reacting a compound of formula (II) or a protected derivative thereof, with a compound of formula (III): HOCH2-Im (III) or a salt thereof in the presence of an acid at an elevated temperature, followed where necessary by removal of any protecting groups.
摘要翻译：本发明提供了制备通式（I）化合物的方法：其中Im表示下式的咪唑基：R 1表示氢原子或本文定义的基团，包括-CO 2 R 5，-COR 5，-CONR 5 R 6或 -SO 2 R 5，其中R 5和R 6可以相同或不同，如本文所定义，条件是当R 1表示-CO 2 R 5或-SO 2 R 5基团时，R 5不表示氢原子; 由R 2，R 3和R 4表示的基团之一是氢原子或C 1-6烷基，C 3-7环烯基，C 3-6烯基，苯基或苯基C 1-3烷基，其它两个基团可以相同或不同的，表示氢原子或C 1-6烷基; n表示2或3; 其包括在酸的存在下在升高的温度下使式（II）化合物或其保护的衍生物与式（III）的化合物或其盐反应，然后在需要时通过除去任何保护基团。

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