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Synthesis of Pyrazoles from 1,3-Diols via Hydrogen Transfer Catalysis

Daniel C. Schmitt*, Alexandria P. Taylor, Andrew C. Flick and Robert E. Kyne, Jr.

*Pfizer Global Research and Development, Eastern Point Road, Groton, Connecticut 06340, United States, Email: daniel.schmittpfizer.com

D. C. Schmitt, A. P. Taylor, A. C. Flick, R. E. Kyne, Jr., Org. Lett., 2015, 17, 1405-1408.

DOI: 10.1021/acs.orglett.5b00266 (free Supporting Information)



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Abstract

Ruthenium-catalyzed hydrogen transfer of 1,3-diols in the presence of alkyl hydrazines provides 1,4-disubstituted pyrazoles. A regioselective synthesis of unsymmetrical pyrazoles from β-hydroxy ketones can also be achieved.

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Key Words

Pyrazoles, Crotononitrile


ID: J54-Y2015