Process for purifying 20(S)-camptothecin

US6476225B2 · kind B2 · utility

Assignee

• BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG · DE

Inventors

• Rainer Sobotta · Ingelheim am Rhein, DE
• Armin Rapp · Gau-Algesheim, DE

Key dates

• Filing date: Jan 17, 2002
• Grant date: Nov 5, 2002
• Expiry date: Jan 17, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

A process for purifying 20(S)-camptothecin, the process comprising:(a) combining an aqueous base and a starting material containing 20(S)-camptothecin to convert the lactone ring of the 20(S)-camptothecin into a carboxylate salt;(b) hydrogenating to the product of step (a) in the presence of a transition metal catalyst;(c) acidifying the aqueous phase of the product of step (b) to form 20(S)-camptothecin crystals;(d) adding at least one polar aprotic solvent to the product of step (c); and(e) separating off the purified 20(S)-camptothecin crystals.