Methods useful in the synthesis of halichondrin B analogs

摘要

In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).

主权项

1. A method of preparing an intermediate in the synthesis of eribulin, said method comprising reacting a compound having formula (I): wherein each of R1, R2, R3, R4, and R5 is independently a silyl group, with a fluoride source in a solvent comprising an amide to produce the intermediate ER-811475: wherein the amide is an N,N C1-C6 dialkyl C1-C6 alkyl amide or N C1-C6 alkyl C2-C6 lactam.