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US 10,308,665 B2Granted
Method for the synthesis of rapamycin derivatives
AssigneeSynbias Pharma AG
InventorsOleksandr Zabudkin, Christian Schickaneder, Iaroslav Matviienko, Volodymyr Sypchenko
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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).
Claims14
Method for the production of a rapamycin derivative of formula (I), comprising:
- (a) preparing a 2-(tri-substituted silyl)oxyethyl triflate of formula 4 by reacting ethylene oxide and a tri-substituted silyl triflate of formula 3
- wherein R1, R2, and R3 are independently selected from the group consisting of C1-C12 alkyl and C1-C12 aryl;
- (b) reacting the 2-(tri-substituted silyl)oxyethyl triflate of formula 4 obtained in step (a) with rapamycin in the presence of a molar excess of organic base to obtain a protected rapamycin derivative of formula 5;
- and
- (c) deprotecting the protected rapamycin derivative of formula 5 to obtain the rapamycin derivative if formula (I).
2 more elements
Dependencies are inferred from the claim text.