Intermediates for producing semi-synthetic penicillins and cepha

Details Intermediates for producing semi-synthetic penicillins and cepha Intermediates for producing semi-synthetic penicillins and cepha

1973-07-12

1977-12-06

Rizzo, Nicholas S.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424271, 424246, 544 22, 544 16, 544 30, C07D50104, C07D49912

Patent

active

040616282

ABSTRACT:
Novel 6-APA, 7-ACA, and 7-ADCA derivatives are described which comprise phosphorylated derivatives of 6-APA, 7-ACA, or 7-ADCA and the corresponding acylated derivatives thereof. The novel 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 and subsequently acylating the thus formed phosphorylated compound, to form a phosphorylated acylated derivative which upon hydrolysis with water splits off the protective group(s) to provide the corresponding semi-synthetic penicillin or cephalosporin having useful antibacterial activity.

REFERENCES:
patent: 3809699 (1974-05-01), Ishimaru

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