Process for the preparation of penam derivatives

Details Process for the preparation of penam derivatives Process for the preparation of penam derivatives

C - Chemistry, Metallurgy

07

D

260/111

C07D 499/72 (2006.01) C07D 499/00 (2006.01)

Patent

CA 1147325

ABSTRACT A process for the preparation of a penam derivative of formula (I): Image (I) wherein R is phenyl, p-hydroxyphenyl, p-(C1-6)-alkyl- carbonyloxyphenyl or 2- or 3-thienyl, R1 is hydrogen, or a pharmaceutically acceptable salt-forming ion or ester-forming radical, and R2 represents hydrogen or a pharmaceutically acceptable salt-forming ion or in vivo hydrolysable ester-forming radical; which process comprises reacting a suitably protected 6,.alpha. arylthio derivative with methanol in the presence of either:(a) silver, thallium or mercuric ions; or (b) chlorine and a base; and thereafter if necessary removing the protecting groups, and converting the product to a pharmaceutically acceptable salt or ester thereof.

361783

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