Bioorganic & medicinal chemistry letters

Facile synthesis of 4-substituted-4-aminopiperidine derivatives, the key building block of piperazine-based CCR5 antagonists

XH Jiang, YL Song, YQ Long

文献索引：Jiang, Xiao-Hua; Song, Yan-Li; Long, Ya-Qiu Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 14 p. 3675 - 3678

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被引用次数: 15

摘要

4-Substituted-4-aminopiperidine is an interesting structural motif found in a number of bioactive compounds. An efficient and convenient method for the synthesis of 4-differently substituted-4-aminopiperidine derivatives was described, employing isonipecotate as a starting material and Curtius rearrangement as a key step. The alkylation of isonipecotate could introduce various substituents at the 4-position of the piperidine ring. With this key ...