Synlett 2020; 31(02): 175-178
DOI: 10.1055/s-0039-1691526
letter
© Georg Thieme Verlag Stuttgart · New York

One-Pot, Metal- and Azide-Free Synthesis of 1,2,3-Triazoles from α-Ketoacetals and Amines

Luke R. Zehnder
a   Oncology Chemistry, Pfizer Medicine Design, 10770 Science Center Drive, San Diego, CA 92121, USA   Email: scott.sutton@pfizer.com
,
Joel M. Hawkins
b   Pharmaceutical Sciences, Pfizer Inc., Eastern Point Road, Groton, CT 06340, USA
,
Scott C. Sutton
a   Oncology Chemistry, Pfizer Medicine Design, 10770 Science Center Drive, San Diego, CA 92121, USA   Email: scott.sutton@pfizer.com
› Author Affiliations
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Publication History

Received: 16 October 2019

Accepted after revision: 19 November 2019

Publication Date:
03 December 2019 (online)


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Abstract

An efficient one-pot two-step synthesis of 1,4-disubstituted 1,2,3-triazoles from α-ketoacetals and amines is presented. The method does not use metals, azides, or oxidants, and is compatible with a variety of functional groups, including heterocycles, esters, nitriles, and carbamates.

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