公开(公告)号：US20060063927A1

公开(公告)日：2006-03-23

申请号：US11229678

申请日：2005-09-20

申请人： Olga Etlin ,  Michael Brand ,  Julia Ditkovich ,  Guy Davidi ,  Moty Shookrun ,  Oded Arad ,  Joseph Kaspi

发明人： Olga Etlin ,  Michael Brand ,  Julia Ditkovich ,  Guy Davidi ,  Moty Shookrun ,  Oded Arad ,  Joseph Kaspi

IPC分类号： C07D498/02

CPC分类号： C07D285/36

摘要： The present invention provides herein a two-step process for preparing pharmaceutically pure quetiapine and salts thereof by obtaining the starting material 11-chloro-dibenzo-thiazepine followed by reacting the 11-chloro-dibenzo-thiazepine with 1-(2-hydroxyethoxy)ethylpiperazine, or its salt, in the presence of an inorganic or organic base in an organic solvent or in a two-phase solvent system. The present invention provides also a novel, one-pot reaction process for preparing pharmaceutically pure quetiapine and salts thereof. The two processes provided herein can be easily, conveniently and inexpensively scaled-up.

摘要翻译： 本发明在此提供了制备药学上纯的喹硫平及其盐的两步法，其方法是通过获得原料11-氯 - 二苯并 - 氮杂，然后将11-氯 - 二苯并噻吖庚因与1-（2-羟基乙氧基）乙基哌嗪 ，或其盐，在无机或有机碱存在下在有机溶剂中或在两相溶剂体系中。 本发明还提供了一种用于制备药学上纯的喹硫平及其盐的新型一锅反应方法。 这里提供的两个方法可以容易地，方便地和低成本地放大。