Intermediate of eribulin and preparation method therefor
AssigneeSelection Bioscience LLC
InventorsFuyao Zhang, Huoming Li, Xinning Zhang
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Abstract
Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1 and R2 is an acetal protecting group or a thioacetal protecting group; R3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.
Claims25
A compound of formula V, VA, VII, VIIA, II, IX or X;
- wherein Ar is an aryl substituted by C1-10 alkyl or alkoxy, or an unsubstituted aryl;
- R1 and R2 are acetal or thioacetal protecting group, and R1 and R2 are each independently C1-10 alkoxy or C1-10 alkylthio, or R1 and R2 together with the carbon atom to which they are attached form cyclic acetal or cyclic thioacetal;
- R3 is methanesulfonyl, p-toluenesulfonyl or trifluoromethanesulfonyl;
- Y is chloride, bromide or iodide;
- and
- X is chloride, bromide, iodide or trifluoromethanesulfonyloxy.
Dependencies are inferred from the claim text.