Palladium catalyzed amination of 2-chloro-1,3-azole derivatives: Mild entry to potent H-1-antihistaminic norastemizole

被引:66
作者
Hong, YP [1 ]
Tanoury, GJ [1 ]
Wilkinson, HS [1 ]
Bakale, RP [1 ]
Wald, SA [1 ]
Senanayake, CH [1 ]
机构
[1] SEPRACOR INC,DEPT PROC RES & DEV,MARLBOROUGH,MA 01752
关键词
D O I
10.1016/S0040-4039(97)01273-2
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Palladium-catalyzed selective amination of 4-fluorobenzyl-2-chlorobenzimidazole with 4-aminopiperidine provided a simple solution for the norastemizole synthesis. Pd-catalyzed amination of other 2-chloro-1,S-Azole derivatives are exploited. (C) 1997 Elsevier Science Ltd.
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页码:5607 / 5610
页数:4
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