Process for preparing 7-(alpha-hydroxy-alpha-phenyl)acetamido-3-(1-methyl-1h-tetrazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid and derivatives thereof
Abstract
Abstract 1. A PROCESS FOR PREPARING A CEPHALOSPORIN OF THE FORMULA 2-(R-OOC-),3-((1-(H3C-)-TETRAZOL-5-YL)-S-CH2-),7-(H5C6- CH(-OH)-CO-NH-)-2-CEPHEM WHICH COMPRISES (1) REACTING A 7-ACYLAMIDO-3-ACTOXYMETHYL COMPOUND OF THE FORMULA 2-(R-OOC-),3-(H3C-COO-CH2-),7-(H-CO-NH-)-2-CEPHEM IN WHICH R IS HYDROGEN OR A CARBOXY PROTECTING GROUP, WITH 1-METHYL-1H-TETRAZOLE-5-THIOL OR AN ALKALIM ALKALINE EARTH METAL OR AMMONIUM SALT THEREOF TO PRODUCE A 7ACYLAMIDO-3-(1 - METHYL-1H-TETRAZOLE-5-YLTHIOMETHYL) COMPOUND OF THE FORMULA 2-(R-OOC-),3-((1-(H3C-)-TETRAZOL-5-YL)-S-CH2-),7-(H-CO- NH-)-2-CEPHEM (2) CLEAVING THE 7-ACYLAMIDO-3-(1-METHYL-1H-TETRAZOL-5YLTHIOMETHYL) COMPOUND TO PRODUCE A 7-AMINO-3-(1-METHYL-1H-TETRAZOL-5-YLTHIOMETHYL) COMPOUND OF THE FORMULA 2-(R-OOC-),3-((1-(H3C-)-TETRAZOL-5-YL)-S-CH2-),7-(H2N-)- 2-CEPHEM AND (3) ACYLATING THE RESULTING 7-AMINO COMPOUND WITH ANHYDRO-O-CARBOXYMANDELIC ACID HAVING THE FORMULA 2,4-DI(O=),5-(H5C6-)-1,3-DIOXOLANE TO PRODUCE THE AFOREMENTIONED CEPHALOSPORIN.
Inventors
- 👤 J Greene
Bibliographic Details
Claims Analysis
Total Claims: 2References Cited (Backward Citations)
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| 3.5 Years (Year 4) | 1977-10-07 | 1978-04-08 | 1978-10-08 | $2000.00 | Window Closed / Lapsed |
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