公开(公告)号：US20120259116A1

公开(公告)日：2012-10-11

申请号：US13516795

申请日：2010-12-20

申请人： Rajiv Kumar ,  Dharmesh Kumar Arvindbhaipatel ,  Dattatray Shamrao Metil ,  Praveen Raosaheb Supekar ,  Prashant Pandurangpawar ,  Santosh Vitthal Pune

发明人： Rajiv Kumar ,  Dharmesh Kumar Arvindbhaipatel ,  Dattatray Shamrao Metil ,  Praveen Raosaheb Supekar ,  Prashant Pandurangpawar ,  Santosh Vitthal Pune

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of 9-O-acylated paliperidone. In a preferred embodiment of the present invention, Paliperidone Form (II) of purity of about 98% or more was obtained by basic hydrolysis of 9-O-Acetyl Paliperidone.

摘要翻译： 本发明涉及一种通过9-O-酰化的利培酮的水解制备普利培酮的新方法。 在本发明的优选实施方案中，通过9-O-乙酰基哌啶酮的碱性水解得到约98％或更高纯度的哌啶酮形式（II）。