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Tandem thiyl radical addition and cyclization of chiral hydrazones using a silicon-tethered alkyne
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Tandem thiyl radical addition and cyclization of chiral hydrazones using a silicon-tethered alkyne

Gregory K Friestad, Tao Jiang and Gina M Fioroni
Tetrahedron: asymmetry, Vol.14(19), pp.2853-2856
2003
DOI: 10.1016/S0957-4166(03)00540-8

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Abstract

A diastereoselective method for addition of a trans-2-(phenylthio)vinyl group to α-hydroxy hydrazones is presented. An ethynyl group, tethered to α-hydroxy hydrazones via a silicon tether, undergoes thiyl radical addition and cyclization under neutral tin-free conditions. In the same pot, desilylation with potassium fluoride or tetrabutylammonium fluoride affords ( E)-vinylsulfides. The one-pot process is the synthetic equivalent of an acetaldehyde Mannich reaction with acyclic stereocontrol. Graphic

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