DR ANTHONY MELVIN CRASTO,WorldDrugTracker, helping millions, A 90 % paralysed man in action for you, I am suffering from transverse mylitis and bound to a wheel chair, With death on the horizon, nothing will not stop me except God
DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 30 Yrs Exp. in the feld of Organic Chemistry. Serving chemists around the world. Helping them with websites on Chemistry.Millions of hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution
n

Sunday 21 September 2014

Metal-free coupling of saturated heterocyclic sulfonylhydrazones with boronic acids



jo-2013-02526z_0011

 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.

No comments:

Post a Comment