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Sunday, 21 September 2014

Metal-free coupling of saturated heterocyclic sulfonylhydrazones with boronic acids


 Department of Chemistry, University of Cambridge, Cambridge, CB2 1EW, U.K.
 Neusentis Chemistry, Pfizer Worldwide Research and Development, The Portway Building, Granta Park, Cambridge, CB21 6GS, U.K.
J. Org. Chem.201479 (1), pp 328–338
DOI: 10.1021/jo402526z

The coupling of aromatic moieties with saturated heterocyclic partners is currently an area of significant interest for the pharmaceutical industry. Herein, we present a procedure for the metal-free coupling of 4-, 5-, and 6-membered saturated heterocyclic p-methoxyphenyl (PMP) sulfonylhydrazones with aryl and heteroaromatic boronic acids. This procedure enables a simple, two-step synthesis of a range of functionalized sp2–sp3 linked bicyclic building blocks, including oxetanes, piperidines, and azetidines, from their parent ketones.

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