Intermediates for producing semi-synthetic penicillins and...

C - Chemistry – Metallurgy – 07 – F

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260/108.5, 260/1

C07F 9/65 (1980.01)

Patent

CA 1040192

ABSTRACT OF THE DISCLOSURE Phosphorylated derivatives of 6-APA, 7-ACA, and 7-ADCA derivatives are described which are intermediates in the preparation of semi-synthetic penicillins and cephalosporins. The compounds are prepared by the reaction of 6-APA, 7-ACA, 7-ADCA or a salt thereof with a phosphorus halide in the presence of an acid acceptor. The phosphorylated derivatives may be acylated to form phosphorylated acylated derivates which upon hydrolysis with water split off the protective group(s) to provide the corresponding semi-synthetic penicillin or cephalo- sporin having useful antibacterial activity.

229385

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