公开(公告)号：US07592459B2

公开(公告)日：2009-09-22

申请号：US11235106

申请日：2005-09-27

申请人： Oded Arad ,  Lior Zelikovitch ,  Mohammed Alnabari ,  Michael Brand ,  Irina Gribun ,  Ada Salman ,  Meital Shiffer ,  Moty Shookrun ,  Orna Kurlat ,  Moshe Bentolila ,  Joseph Kaspi

发明人： Oded Arad ,  Lior Zelikovitch ,  Mohammed Alnabari ,  Michael Brand ,  Irina Gribun ,  Ada Salman ,  Meital Shiffer ,  Moty Shookrun ,  Orna Kurlat ,  Moshe Bentolila ,  Joseph Kaspi

IPC分类号： C07D211/02

CPC分类号： C07D211/32

摘要： The present invention provides a crystalline donepezil maleate, which is used as an intermediate in the preparation of donepezil hydrochloride. Also provided are novel processes for producing same in substantially pure form and a process for producing pharmaceutically pure amorphous donepezil hydrochloride therefrom.

摘要翻译： 本发明提供结晶的多奈哌齐马来酸盐，其用作制备盐酸多奈哌齐中的中间体。 还提供了用于以基本上纯的形式生产其的新方法和由其制备药学上纯的无定形多奈哌齐盐酸盐的方法。

公开(公告)号：US20060069263A1

公开(公告)日：2006-03-30

申请号：US11233096

申请日：2005-09-23

申请人： Irina Gribun ,  Ada Salman ,  Meital Shiffer ,  Moty Shookrun ,  Michael Brand ,  Oded Arad ,  Joseph Kaspi

发明人： Irina Gribun ,  Ada Salman ,  Meital Shiffer ,  Moty Shookrun ,  Michael Brand ,  Oded Arad ,  Joseph Kaspi

IPC分类号： C07D277/82

CPC分类号： C07D277/62

摘要： A process is disclosed for the reduction of (S)-2-amino-6-propionamido-4,5,6,7-tetrahydrobenzothiazole, which comprises reacting (S)-2-amino-6-propionamido-4,5,6,7-tetrahydrobenzothiazole with a borane reagent in the presence of suitable organic solvent to yield (S)-2-amino-6-propylamino-4,5,6,7-tetrahydrobenzothiazole base, which may be converted to an acid addition salt thereof. The process provided herein can be easily, conveniently and inexpensively scaled-up.

摘要翻译： 公开了用于还原（S）-2-氨基-6-丙酰胺基-4,5,6,7-四氢苯并噻唑的方法，其包括使（S）-2-氨基-6-丙酰胺基-4,5,6 ，7-四氢苯并噻唑与硼烷试剂在合适的有机溶剂存在下反应，得到（S）-2-氨基-6-丙基氨基-4,5,6,7-四氢苯并噻唑碱，其可以转化为其酸加成盐 。 本文提供的方法可以容易地，方便地和低成本地放大。

公开(公告)号：US20060069125A1

公开(公告)日：2006-03-30

申请号：US11235106

申请日：2005-09-27

申请人： Oded Arad ,  Lior Zelikovitch ,  Mohammed Alnabari ,  Michael Brand ,  Irina Gribun ,  Ada Salman ,  Meital Shiffer ,  Moty Shookrun ,  Orna Kurlat ,  Moshe Bentolila ,  Joseph Kaspi

发明人： Oded Arad ,  Lior Zelikovitch ,  Mohammed Alnabari ,  Michael Brand ,  Irina Gribun ,  Ada Salman ,  Meital Shiffer ,  Moty Shookrun ,  Orna Kurlat ,  Moshe Bentolila ,  Joseph Kaspi

IPC分类号： A61K31/445 ,  C07D211/06

CPC分类号： C07D211/32

摘要： The present invention provides a crystalline donepezil maleate, which is used as an intermediate in the preparation of donepezil hydrochloride. Also provided are novel processes for producing same in substantially pure form and a process for producing pharmaceutically pure amorphous donepezil hydrochloride therefrom.