公开(公告)号：EP1700843A3

公开(公告)日：2010-02-24

申请号：EP06013053.1

申请日：2001-07-26

Applicant: Shire US Inc.

Inventor： Lang, Philip Charles ,  Spencer, Roxanne Paula ,  Yeh, Wen-Lung ,  Roth, Michael Jopseph

IPC: C07C209/36 ,  C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C201/14

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making certain 6,7-dihalo-1,5-dihydroimidazo [2,1-b] quinazolin-2(3H)-ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6-nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnCl 2 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones from the corresponding iminoquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.

公开(公告)号：EP1700843A2

公开(公告)日：2006-09-13

申请号：EP06013053.1

申请日：2001-07-26

Applicant: Shire US Inc.

Inventor： Lang, Philip Charles ,  Spencer, Roxanne Paula ,  Yeh, Wen-Lung ,  Roth, Michael Jopseph

IPC: C07C209/36 ,  C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C201/14

CPC classification number: C07D487/04 ,  C07C201/08 ,  C07C201/12 ,  C07C227/04 ,  C07C227/16 ,  C07C229/16 ,  C07C205/12 ,  C07C205/26 ,  C07C205/44

Abstract: Methods are provided for making certain 6,7-dihalo-1,5-dihydroimidazo [2,1-b] quinazolin-2(3H)-ones from 2,3-dihalobenzaldehydes. A method is also provided for making the intermediate ethyl N-(2,3-dihalo-6-nitrobenzyl)glycines from 2,3-dihalobenzaldehydes and for reducing the glycine compounds using either SnCl 2 or a specially defined catalyst. A cyclization method to form the desired 6,7-dihalo-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-ones from the corresponding iminoquinazoline compounds is further provided. These methods are particularly suitable in the manufacture of Anagrelide base.

Abstract translation: 提供了从2,3-二卤代苯甲醛制备某些6,7-二卤代-1,5-二氢咪唑并[2,1-b]喹唑啉-2（3H） - 酮的方法。 还提供了从2,3-二卤代苯甲醛制备中间体N-（2,3-二卤代-6-硝基苄基）甘氨酸和使用SnCl2或特定催化剂还原甘氨酸化合物的方法。 进一步提供从相应的亚氨基喹唑啉化合物形成所需的6,7-二卤代-1,5-二氢咪唑并[2,1-b]喹唑啉-2（3H） - 酮的环化方法。 这些方法特别适用于制造阿那格雷碱。