A CONVERGENT SYNTHESIS OF 4-(2-BENZOTHIAZOYL)PIPERIDINES WITH ANTIHISTAMINIC ACTIVITY

被引:8
作者
MAYNARD, GD
CHENG, HC
KANE, JM
STAEGER, MA
机构
[1] Marion Merrell Dow Research Institute, Cincinnati, OH 45215-6300
关键词
D O I
10.1016/S0960-894X(01)81268-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of 4-(N-methoxy-N-methylcarboxamido)-1-piperidinecarboxylic acid 1,]-dimethylethyl ester (5) is described. Reaction of this intermediate with 2-lithiobenzothiazole followed by deprotection and N-alkylation yields a series of 4-(2-benzothiazoyl)piperidines with potent antihistaminic activity.
引用
收藏
页码:753 / 756
页数:4
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