Claims
- 1. A process for the preparation of cephalosporin derivatives represented by the following general formula (V) or pharmacologically acceptable salts thereof: ##STR12## wherein R.sub.1 stands for a p-hydroxyphenyl group or a cyanomethylthio group, R.sub.2 stands for a hydrogen atom or an amino or protected amino group, R.sub.3 stands for a 1H-1,2,3-triazol-5-ylthio group or a 1-methyl-1,2,3,4-tetrazol-5-ylthio group, and R.sub.4 stands for a hydrogen atom or a methoxy group, which comprises reacting a 7-aminocephalosporin derivative represented by the following general formula (IV) or a salt thereof: ##STR13## wherein R.sub.4 is as defined above and R.sub.5 stands for a halogen atom, an azido group, an acetoxy group or a benzimidazolylthio group, with a thioester compound represented by the following general formula (I): ##STR14## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above, in the presence of a solvent.
- 2. A process according to claim 1, wherein said thioester represented by the general formula (I) is employed in an amount of 1.0 to 2.0 mols per mol of said 7-aminocephalosporin derivative represented by the general formula (IV).
- 3. A process according to claim 1, wherein R.sub.5 stands for an acetoxy group.
- 4. A process according to claim 1, wherein R.sub.5 stands for a benzimidazolylthio group and the reaction is carried out in the presence of an acid catalyst.
- 5. A process according to claim 4, wherein the acid catalyst is hydrochloric acid or sulfuric acid.
- 6. A process according to claim 4, wherein the solvent is an aprotic polar solvent or water-containing aprotic polar solvent.
- 7. A process according to claim 6, wherein the aprotic polar solvent is N,N-dimethylformamide or N,N-dimethylacetamide.
- 8. A process as set forth in claim 1, wherein R.sub.1 stands for a p-hydroxyphenyl group, R.sub.2 stands for an N-carbobenzyl-oxyamino group and R.sub.3 stands for a 1H-1,2,3-triazol-5-ylthio group.
- 9. A process as set forth in claim 1, wherein R.sub.1 stands for a cyanomethylthio group, R.sub.2 stands for a hydrogen atom and R.sub.3 stands for a 1-methyl-1,2,3,4-tetrazol-5-ylthio group.
Priority Claims (6)
Number |
Date |
Country |
Kind |
55-120619 |
Sep 1980 |
JPX |
|
55-121718 |
Sep 1980 |
JPX |
|
55-142048 |
Oct 1980 |
JPX |
|
55-146859 |
Oct 1980 |
JPX |
|
55-148178 |
Oct 1980 |
JPX |
|
56-108797 |
Jul 1981 |
JPX |
|
Parent Case Info
This is a division of application Ser. No. 298,884, filed Sept. 2, 1981.
US Referenced Citations (5)
Divisions (1)
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Number |
Date |
Country |
Parent |
298884 |
Sep 1981 |
|