Process for the preparation of 7-acylamino-3-(thio-...

Details Process for the preparation of 7-acylamino-3-(thio-... Process for the preparation of 7-acylamino-3-(thio-...

C - Chemistry, Metallurgy

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C07D 501/36 (2006.01) C07D 499/00 (2006.01) C07F 7/08 (2006.01) C07F 7/10 (2006.01) C07F 7/18 (2006.01) C07F 9/24 (2006.01) C07H 23/00 (2006.01) C07J 51/00 (2006.01)

Patent

CA 1176241

ABSTRACT OF THE DISCLOSURE Process for the preparation of 7-acylamino-3- (thio-substituted)methyl-3-cephem-4-carboxylic acid 1- oxide derivatives by reacting a 7-acylamino-3-bromomethyl- 3-cephem-4-carboxylic acid l-oxide derivative with a silylated thiol of the general formula: R - S - Si(CH3)3 wherein R represents an organie group, preferably a 5- or 6-membered heterocyelie group, which reaction is preferably earried out in the presence of an inert organie solvent at a temperature between -20° and 80°C thereby obtaining the eorresponding 7-acylamino-3-(R- thiomethyl)-3-eephem-4-earboxylic acid l-oxide derivatives, many of whieh are valuable intermediates in methods for the preparation of therapeutieally aetive cephalosporins.

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