Process for the preparation of rapamycin derivatives

US8138344B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Murat Acemoglu · Basel, CH
• Sabine Pfeffer · Weil am Rhein, DE

Key dates

• Filing date: Jan 22, 2007
• Grant date: Mar 20, 2012
• Expiry date: May 6, 2029

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P37/06
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Processes for the production of a 32-deoxorapamycin from a 32-iodo- or 32-hydroxyrapamycin, wherein the hydroxy group is substituted by the residue of an arylthionocarbonate or an arylthiocarbamate, in the presence of tris(trimethylsilyl)-silan and α,α′-azo-isobutyronitril in organic solvent; and 32-deoxorapamycin in the form of a crystalline solvate.