4.8 Article

An efficient direct amination of cyclic amides and cyclic ureas

Journal

ORGANIC LETTERS
Volume 8, Issue 11, Pages 2425-2428

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol060815y

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[graphics] An efficient one-step amination of cyclic amides and ureas has been developed. Treatment of cyclic amides and cyclic ureas with BOP in the presence of DBU in various solvents led to the formation of cyclic amidines and cyclic guanidines in good to excellent yields. Concise syntheses of biologically intriguing kinetin and potent kinase inhibitor olomoucin were thus achieved in just one and two steps, respectively.

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