Process for the cleavage of cephalosporin prodrug esters to 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid

US5410042A · kind A · utility

Assignee

• Hoechst GmbH · DE

Inventors

• Norbert Krass · Frankfurt am Main, DE
• Elisabeth Defossa · Idstein, DE
• Gerd Fischer · Limburg, DE
• Uwe Gerlach · Hattersheim, DE
• Rolf-Ludwig HOERLEIN · Frankfurt am Main, DE
• Rudolf Lattrell · Königstein, DE
• Adolf Linkies · Frankfurt, DE
• Wolfgang Martin · Ludwigshafen, DE
• Ulrich Stache
• Theodor Wollmann · Hofheim, DE

Key dates

• Filing date: May 19, 1993
• Grant date: Apr 25, 1995
• Expiry date: May 19, 2013

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D501/00
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention relates to a process for the preparation of 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid (I) from 7-amino-3-methoxymethylceph-3-em-4-carboxylic acid esters (II) or their salts by ester cleavage. The process comprises treating the compound II with formic acid, trifluoroacetic acid, methanesulfonic acid or trifluoromethanesulfonic acid or a mixture of two of these acids in each case.