Process Development of Halaven (R): Synthesis of the C1-C13 Fragment from D-(-)-Gulono-1,4-lactone

[摘要]：A 12-step kilogram-scale synthesis of the C1-C13 fragment, common to halichondrin B and the totally synthetic analogue Halaven (R) (E7389, INN eribulin mesylate), is described. The synthesis features four crystalline intermediates which facilitates throughput, and enhances quality control of all stereogenic centers in the title compound.

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