Patent · US Expired

Process for the preparation of 7-aminocephalosporanic acids

US3932392A · kind A · utility

10Cited by
2References
11Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJan 14, 1974
Grant dateJan 13, 1976
Priority date
Expiry dateJan 14, 1994

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D501/18
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

7-Aminocephalosporanic acid (7-ACA) and 7-amino-3-methyl-3-cephem-4-carboxylic acid (7-ADCA) are valuable intermediates in the preparation of semi-synthetic cephalosporins. These compounds are commonly prepared by cleaving the amide bond of compounds having the formula ##SPC1## In which R.sup.6 is H or ##EQU1## R is the side chain of a known penicillin, especially phenoxymethyl or benzyl, and the amino and carboxyl functions are blocked; by A. halogenating the blocked compounds Ia or IIa to produce an imino-halide; B. forming an imino-ether from the imino-halide by treatment with an alcohol; and C. mixing said imino-ether with water or an alcohol to produce 7-aminocephalosporanic acid or 7-amino-3-methyl-3-cephem-4-carboxylic acid. The invention claimed is the use of dicyclohexylamine or diisopropylamine instead of a tertiary amine acid scavenger in step A.

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