摘要
以N,N-双(2-氯乙基)氨基盐酸盐为原料,经加保护基、碳烷基化、水解脱羧3步反应合成1-叔丁基氧羰基-4-(2-吡啶基)哌啶,总收率为64.66%。该方法操作简便、收率高且具有通用性,可用来合成4-(3-吡啶基)哌啶、4-(2-吡啶基)四氢吡喃等多种化合物。
tert-Butyl-4-(pyridin-2-yl)piperidine-l-carboxylate was synthesized from bis hydrochloride and 2-(pyridin-2-yl)acetonitrile as raw material by group-protecting,C-alky (2-chloroethyl) amine lation, hydrolysis and decarboxylation. The total yield reached 64.66%. Particularly, the method has advantages such as easy operation, high yield, high versatility, and can be used to synthesize 4- (pyridin-3-yl) piperidine, 4- (pyridin-2-yl) tetrahydropyran and other compounds.
出处
《化学与生物工程》
CAS
2014年第4期24-25,28,共3页
Chemistry & Bioengineering
基金
教育部归国留学人员科研基金资助项目(201000265)
关键词
碳烷基化
脱羧
哌啶
C-alkylation
decarboxylation
piperidine