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. 2012 Apr 6;14(7):1752-5.
doi: 10.1021/ol300352z. Epub 2012 Mar 14.

Formal nucleophilic substitution of bromocyclopropanes with azoles

Pavel Ryabchuk  1 , Marina Rubina, Jack Xu, Michael Rubin
Affiliations

Formal nucleophilic substitution of bromocyclopropanes with azoles

Pavel Ryabchuk et al. Org Lett. .

Abstract

A highly diastereoselective protocol for the formal nucleophilic substitution of 2-bromocyclopropylcarboxamides with azoles is described. A wide range of azoles, including pyrroles, indoles, benzimidazoles, pyrazoles, and benzotriazoles, can be efficiently employed as pronucleophiles in this transformation, providing expeditious access to N-cyclopropyl heterocycles.

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