Patent · US Expired

3-Substituted amino-cephalosporins

US4013651A · kind A · utility

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10Claims
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Assignee

Inventor

Key dates

Filing dateMay 12, 1975
Grant dateMar 22, 1977
Priority date
Expiry dateMay 12, 1995

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D501/59
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

7-Amino-(or 7-acylamido)-3-(disubstituted-amino)-3-cephem-4-carboxylic acid esters are prepared with the corresponding 3-chloro-3-cephem ester or 3-alkyl-(or aryl)-sulfonyloxy-3-cephem esters and a secondary amine, e.g., diphenylmethyl 7-[2-(2-thienyl)acetamido] -3-morpholino-3-cephem-4-carboxylate is prepared with the corresponding 3-methyl-sulfonyloxy ester and morpholine. The 3-amino-substituted cephem esters are useful intermediates undergoing reduction with diborane to the corresponding 3H-3-cephem esters, or, alternatively, they are reacted with Grignard reagents, e.g., phenylmagnesium bromide to provide, for example, the 3-phenyl-3-cephem ester.

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