I₂-TBHP-catalyzed oxidative cross-coupling of N-sulfonyl hydrazones and isocyanides to 5-aminopyrazoles.

Org Lett

†Department of Medicinal and Applied Chemistry, Kaohsiung Medical University, No. 100, Shih-Chuan First Rd, Sanmin District, Kaohsiung City, 807, Taiwan.

Published: March 2015

I2-TBHP-catalyzed oxidative cross coupling of N-sulfonyl hydrazones with isocyanides has been realized for the synthesis of 5-aminopyrazoles through formal [4 + 1] annulation via in situ azoalkene formation. Notable features are the metal/alkyne-free strategy, C-C and C-N bond formation, atom economy, catalytic I2, broad functional group tolerance, good reaction yields, shorter time, and also applicability to one-pot methodology.

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http://dx.doi.org/10.1021/acs.orglett.5b00398DOI Listing

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