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US 9,434,744 B2Granted
Low temperature synthesis of rapamycin derivatives
AssigneeBiosensors International Group, Ltd.
InventorsMargaret W. Kayo, Richard S. Fornicola, Ivan Kovacik
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Abstract
The present invention provides improved processes for obtaining rapamycin derivatives including Biolimus A9.
Claims18
A method for obtaining a compound having the structure of Formula I
- the method comprising:
- a) combining in a reaction mixture an organic solvent, an organic base compound having a nitrogen heteroatom, a compound having the structure of Formula II
- and
- a compound having the structure of Formula III
- b) maintaining the reaction mixture at a temperature of from 25° C. to 55° C.;
- and
- c) separating from the reaction mixture a compound having the structure of Formula I;
- wherein
- R1 is (CH2)e—O—(CH2)f—H;
- e is an integer selected from 1-5;
- f is an integer selected from 1-5;
- and
- R2 is hydrogen;
- thereby obtaining a compound having the structure of Formula I.
11 more elements
Dependencies are inferred from the claim text.