Method for the synthesis of rapamycin derivatives

US10308665B2 · kind B2 · utility

Assignee

• SYNBIAS PHARMA AG · CH

Inventors

• Oleksandr Zabudkin · Enzklösterle, DE
• Christian Schickaneder · Achern, DE
• Iaroslav Matviienko · Mannheim, DE
• Volodymyr Sypchenko · Mannheim, DE

Key dates

• Filing date: Jun 22, 2016
• Grant date: Jun 4, 2019
• Expiry date: Jun 22, 2036

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D498/18
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention relates to a method for the production of a rapamycin derivative of formula (I), the method comprising the preparation of a 2-(tri-substituted silyl)oxyethyl triflate by reacting ethylene oxide and a tri-substituted silyl triflate, reaction of the resulting 2-(tri-substituted silyl)oxyethyl triflate with rapamycin in the presence of a molar excess of organic base, and deprotection to obtain the rapamycin derivative of compound (I).