Preparation of Heterocyclic Amines via a Copper(I)-Mediated Oxidative Cross-Coupling of Organozinc Reagents with Lithium Amides

[摘要]：Functionalized heteroaromatic amines are readily prepared by the oxidative coupling of polyfunctional zinc amidocuprates using PhI(OAc)(2) as oxidant. Various sensitive heterocyclic organometallics undergo this oxidative cross-coupling reaction furnishing aminated heteroaromatics. A high functional group tolerance and relative insensibility to steric hindrance characterize this general amination reaction. A practical procedure for the preparation of protected primary and secondary as well as tertiary heteroaryl amines is described.

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