| 摘要 |
<p>This invention relates to a method of purifying the antibacterial agent, 7-D-.alpha.-amino-.alpha.-p-hydroxyphenyl)acetamido!-3-(1,2,3-triazol- 5-ylthiomethyl)-3-cephem-4-carboxylic acid by converting said substance into a novel crystalline solvate which is highly suitable for oral and parenteral administration. The duel problems confronting applicants were the need for a practical method for purifying this compound to the high degree necessary for human use and the provision of a form of this drug which could be formulated and administered both orally and parenterally in an aqueous suspension without loss of biological activity and without deleterious changes on standing such as losing crystallinity, not suspending evenly, oiling, clumping, settling out and becoming tacky. 7-D-.alpha.-amino-.alpha.-p-hydroxyphenyl)acetamido!-3-(1,2,3-triazol- 5-ylthiomethyl)-3-cephem-4-carboxylic acid is a new cephalosporin, also called BL-S640, which was described by David Willner and Leonard Bruce Crast, Jr. This specification discloses a process for the preparation of 7-D-.alpha.-amino-.alpha.-p-hydroxyphenyl)acetamido!-3-(1,2,3-triazol- 5-ylthiomethyl)-3-cephem-4-carboxylic acid 1,2-propylene glycolate characterized by adjusting upward the pH of an acidic solution having a pH below about 2.0 of 7-D-.alpha.-amino-.alpha.-p-hydroxyphenyl) acetamido!-3-(1,2,3-triazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid or a hydrate or solvate thereof, in aqueous 1,2-propylene glycol by the addition of a base to raise the pH to at least 4.0 thus precipitating the propylene glycolate product which is then recovered.</p> |
