Process for the preparation of new intermediates useful in the synthesis of cephalosporins
US5945414A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 2, 1997 |
| Grant date | Aug 31, 1999 |
| Priority date | — |
| Expiry date | Dec 2, 2017 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/04
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: ##STR1## with a compound of formula (II): EQU R--SH (II) wherein R is 5-methyl-1,3,4-thiadiazol-2-yl, 1H-1,2,3-triazol-4-yl, 1-methyl-tetrazol-5-yl or PA1 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl group, and R.sup.1 and R.sup.2 are both hydrogen and the other is an acyl group, in an aqueous solution in an amount of 3-5 mols per mol of glutaryl 7-ACA to about 90.degree. C. and for a time from about 2 to about 10 hours; PA1 optionally recovering the excess of the compound of formula (II), thereby preparing a compound of formula (III) in an aqueous solution: ##STR2## wherein R is as above defined and optionally deacylating said compound of formula (III); and PA1 converting the resulting compound of formula (I) ##STR3## wherein R, R.sup.1 and R.sup.2 are as defined above in the presence of a non-chlorinated solvent into one of said cephalosporins.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.