Preparation of penicillanic acid derivatives

Details Preparation of penicillanic acid derivatives Preparation of penicillanic acid derivatives

1980-03-24

1982-08-31

Rizzo, Nicholas S.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

424270, C07D49900

Patent

active

043471820

ABSTRACT:
The compound 6-.beta.-chloropenicillanic acid can be prepared in substantially pure form and is a .beta.-lactamase inhibitor which may be used to enhance the effectiveness of penicillins acid cephalosporins against .beta.-lactamase producing lacteria.
The process comprises the reaction of a compound of the formula: ##STR1## wherein R.sup.X is hydrogen or a carboxyl-blocking group and R is an aryl group, with a trialkyl tin hydride or a triaryl tin hydride or a dialkyl tin dihydride and optionally removing any carboxyl-blocking group R.sup.X, and/or oxidizing the atoms to an SO or SO.sub.2 ; and/or esterifying a salt of the acid to yield an in-vivo hydrolysable ester.

REFERENCES:
patent: 4180506 (1979-12-01), Oratt
patent: 4203992 (1980-05-01), Gordon et al.
JCS Oerkin 1, 1976, p. 704.

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