Novel and Versatile Synthesis of Disubstituted 1,2-Dihydro-1,2,4-triazol-3-ones

Graham, Mark A.; Bethel, Paul A.; Burgess, Jonathan; Fairley, Gary; Glossop, Steve C.; D. R. Greenwood, Ryan; Jones, Clifford D.; Lovell, Scott; Swallow, Steve

doi:10.1021/ol402920z.s002

ol402920z_si_002.pdf (1.97 MB)

Novel and Versatile Synthesis of Disubstituted 1,2-Dihydro-1,2,4-triazol-3-ones

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posted on 2013-12-06, 00:00 authored by Mark A. Graham, Paul A. Bethel, Jonathan Burgess, Gary Fairley, Steve C. Glossop, Ryan D. R. Greenwood, Clifford D. Jones, Scott Lovell, Steve Swallow

A novel method for the synthesis of a wide range of 1,5-disubstituted 1,2-dihydro-1,2,4-triazol-3-ones is described. The key step involves a reaction between a dilithiated BOC-hydrazine and a N-alkoxycarbonylcarboximidothioate. A broad range of aryl and alkyl functional groups are tolerated, providing a versatile route for the synthesis of triazolones.

Novel and Versatile Synthesis of Disubstituted 1,2-Dihydro-1,2,4-triazol-3-ones

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