Intermediates for 6-(aminoacyloxymethyl) penicillanic acid 1,1-d

Details Intermediates for 6-(aminoacyloxymethyl) penicillanic acid 1,1-d Intermediates for 6-(aminoacyloxymethyl) penicillanic acid 1,1-d

1984-12-03

1986-05-27

Rizzo, Nicholas S.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

514196, 514197, 424114, C07D49900, A61K 31425

Patent

active

045914591

ABSTRACT:
beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.

REFERENCES:
patent: 4287181 (1981-09-01), Kellogg
patent: 4342768 (1982-08-01), Kellogg
Greene, Protective Group in Organic Chemistry, p. 239 (1981).

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