公开(公告)号：US07847094B2

公开(公告)日：2010-12-07

申请号：US11808360

申请日：2007-06-08

申请人： Ashok Kumar ,  Dharmendra Singh ,  Swapnali Hemant Patil ,  Ganesh Devidas Mahale ,  Uttamrao Arjunrao Sawant ,  Balasaheb Ganpat Jadhav ,  Ragneshkumar Rana

发明人： Ashok Kumar ,  Dharmendra Singh ,  Swapnali Hemant Patil ,  Ganesh Devidas Mahale ,  Uttamrao Arjunrao Sawant ,  Balasaheb Ganpat Jadhav ,  Ragneshkumar Rana

IPC分类号： C07D281/16

CPC分类号： C07D281/16

摘要： Disclosed herein is an industrial preparation of Quetiapine by the reaction of 11-piperazinyldibenzo[b,f][1,4]-thiazepine or its salt with 2-(2-chloroethoxy)ethanol in presence of an organic or inorganic base under neat or aqueous condition to form 11-[4-{2-(2-hydroxyethoxy)ethyl}-1-piperazinyl]dibenzo[b,f]-[1,4]thiazepine. The quetiapine free base obtained is further converted to its hemi-fumarate salt.

摘要翻译： 本文公开的是在有机或无机碱存在下，在纯净或无机碱存在下，通过11-哌嗪基二苯并[b，f] [1,4] - 噻嗪或其盐与2-（2-氯乙氧基）乙醇的反应， 形成11- [4- {2-（2-羟基乙氧基）乙基} -1-哌嗪基]二苯并[b，f] - [1,4]硫杂吖庚因。 获得的喹硫平游离碱进一步转化为其半富马酸盐。