Patent · US Expired

Sulphur analogs of cephalosporins having a nucleophile substituted in the 7 position

US4381300A · kind A · utility

3Cited by
11References
15Claims
0Family size

Assignee

Inventors

Key dates

Filing dateFeb 3, 1981
Grant dateApr 26, 1983
Priority date
Expiry dateFeb 3, 2001

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D499/00
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Biologically active sulfur analogs of 6-aminopenicillanic acid having a nucleophile substituted in the 6- position are made by reacting a sulfenyl chloride with esters of diazopenicillanic acid. Biologically active sulfur analogs of 7-aminocephalosporanic acid having a nucleophile substituted in the 7- position are analogously made by reacting a sulfenyl chloride with esters of 7-diazocephalosporanic acid. Deacetoxycephalosporins can be formed from the corresponding analog of 6-aminopenicillanic acid and derivations thereof, by sulfoxide rearrangement of the thiazolidine ring of penicillins to the dihydrothiazine ring of cephalosporins. These nucleophile substituted sulfur analogs of penicillins and cephalosporins are new antibacterial agents and display antibacterial activity against a variety of microorganisms.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.