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US 8,742,080 B2Granted
Process for the glycosidation of colchicine and thiocolchicine
AssigneeIndena S.p.A.
InventorsStephen Beszant, Bruno Gabetta
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Abstract
A process for the preparation of compounds having formula (I) is disclosed, wherein: —R1 is a methoxy or methylthio group; —R2 is a O-glycosyloxy residue. Compounds having formula (I) are prepared by reacting the corresponding precursor having R2═OH and the suitably protected 1-acetyl-glycose.
Claims8
A process to prepare compounds having formula I:
- wherein:
- R1 is a methoxy or a methylthio group;
- R2 is a O-glycosyloxy residue;
- said process comprising reacting a protected 1-acetyl-glycose with a compound having formula II:
- wherein R1 is as defined above in the presence of a Lewis acid and an organic base, removing the protecting groups from the glycosyl moiety;
- and obtaining compounds having formula I.
3 more elements
Dependencies are inferred from the claim text.