Process for the preparation of penam derivatives

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

1982-07-09

1985-02-26

Rizzo, Nicholas S.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

2602391, 2602452T, C07D49904, A61K 31425

Patent

active

045016968

ABSTRACT:
A process for the preparation of a penam derivative of formula (I): ##STR1## wherein R.sup.A is hydrogen or a group of formula (Ia): ##STR2## wherein X is --CO.sub.2 R.sup.1, or SO.sub.3 R.sup.1 ; R is C.sub.1-6 alkyl, aryl, or heterocyclyl; R.sup.1 is hydrogen, or a pharmaceutically acceptable salt-forming ion or ester-forming radical, and R.sup.2 represents hydrogen or a pharmaceutically acceptable salt-forming ion or in vivo hydrolyzable ester-forming radical; which process comprises reacting a compound of formula (II): ##STR3## wherein R.sup.B is hydrogen, a removable amino blocking group, or a group of formula (IIa): ##STR4## wherein Y is --CO.sub.2 R.sup.x or --SO.sub.3 R.sup.x ; R is as defined with respect to formula (I) above; R.sup.x represents an ester-forming radical, R.sup.Y represents hydrogen, a salt-forming radical or a carboxyl-blocking group, and R.sup.3 represents an alkyl, benzyl, or aryl group; with methanol in the presence of copper ions; and thereafter if necessary carrying out one or more of the following steps:

REFERENCES:
patent: 3897424 (1975-07-01), Kippel et al.
patent: 3910902 (1975-10-01), Dolfini et al.
patent: 3954731 (1976-05-01), Spitzer et al.
patent: 4048320 (1977-09-01), Clayton et al.
patent: 4062842 (1977-12-01), Dolfini et al.
patent: 4260625 (1981-04-01), Hardy et al.
patent: 4308259 (1981-12-01), Bentley

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