发明名称 |
AHU-377 INTERMEDIATES AND METHOD FOR PREPARING AHU-377 AND AHU-377 INTERMEDIATES |
摘要 |
Disclosed are AHU-377 intermediates and a method for preparing AHU-377 and AHU-377 intermediates. The above-mentioned method for preparing AHU-377 uses a chiral glycidyl benzyl ether as the starting raw material. Intermediate compound (3) is produced by an addition reaction with a biphenyl Grignard reagent and a Mitsunobu reaction with a succimide or a phthalimide. Intermediate compound (4) is obtained after the benzyl protection has been removed. Intermediate compound (4) is oxidised to form an aldehyde, and then is reacted with a phosphorus ylide reagent to obtain target intermediate compound (8). Intermediate (9) is obtained under a selective catalytic hydrogenation condition. Target compound (10), i.e. AHU-377, is obtained by the hydrolysis of the single amide bond. The use of an expensive non-natural amino acid raw material tyrosine can be avoided in the method of the present application, and the method has a convenient operation and high safety. |
申请公布号 |
WO2016180275(A1) |
申请公布日期 |
2016.11.17 |
申请号 |
WO2016CN81244 |
申请日期 |
2016.05.06 |
申请人 |
SUZHOU PENGXU PHARMATECH CO., LTD. |
发明人 |
WANG, Peng;LI, Pixu;GU, Xiangyong |
分类号 |
C07C233/47;C07C41/30;C07C43/178;C07C231/08;C07C269/04;C07C271/16;C07D207/404 |
主分类号 |
C07C233/47 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|