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Org Lett. 2016 Jan 4;18(1):16-9. doi: 10.1021/acs.orglett.5b02994. Epub 2015 Dec 15.

Direct, Regioselective N-Alkylation of 1,3-Azoles.

Author information

1
Medicinal Chemsitry Department, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.

Abstract

Regioselective N-alkylation of 1,3-azoles is a valuable transformation. Organomagnesium reagents were discovered to be competent bases to affect regioselective alkylation of various 1,3-azoles. Counterintuitively, substitution selectively occurred at the more sterically hindered nitrogen atom. Numerous examples are provided, on varying 1,3-azole scaffolds, with yields ranging from 25 to 95%.

PMID:
26671035
DOI:
10.1021/acs.orglett.5b02994
[Indexed for MEDLINE]

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