公开(公告)号：EP0070103A1

公开(公告)日：1983-01-19

申请号：EP82303111.7

申请日：1982-06-16

申请人： BEECHAM GROUP PLC

发明人： Dales, John Robert Mansfield ,  Vallance, Marguerita Anne

IPC分类号： C07D499/04

CPC分类号： C07D499/00

摘要： A process for the preparation of a penam derivative of formula (I):
wherein R A is hydrogen or a group of formula (la):
wherein X is -C0 2 R', or S0 3 R'; R is C 1-6 alkyl, aryl, or heterocyclyl; R' is hydrogen, or a pharmaceutically acceptable salt-forming ion or ester-forming radical, and R 2 represents hydrogen or a pharmaceutically acceptable salt-forming ion or in vivo hydrolysable ester-forming radical; which process comprises reacting a compound of formula (II):
wherein R B is hydrogen, a removable amino blocking group, or a group of formula (Ila):
wherein Y is -CO 2 R x or -SO 3 R x ; R is as defined with respect to formula (I) above; R x represents an ester-forming radical, R y represents hydrogen, a salt-forming radical or a carboxyl-blocking group, and R 3 represents an alkyl, benzyl, or aryl group; with methanol in the presence of copper ions; and thereafter if necessary carrying out one or more of the following steps:

(i) removal of any blocking group;
(ii) converting the product to a pharmaceutically acceptable salt or ester thereof.

公开(公告)号：EP0070103B1

公开(公告)日：1985-05-29

申请号：EP82303111.7

申请日：1982-06-16

申请人： BEECHAM GROUP PLC

发明人： Dales, John Robert Mansfield ,  Vallance, Marguerita Anne

IPC分类号： C07D499/04

CPC分类号： C07D499/00