Preparation of anticancer-active tricyclic compounds via alkyne coupling reaction

摘要

The present invention is directed to provide a novel preparation of anticancer-active tricyclic compounds via alkyne coupling reaction. The present invention provides a process for preparing a compound of formula (Ia) or (Ib):; wherein R¹ is optionally substituted C_1-6 alkyl, etc.; W is O, S or NR²; R² is hydrogen atom, etc., which comprises Step (a) in which a compound of formula (II): ; wherein R¹ is the same as defined above, and a compound of formula (III) or (IV): ; wherein R² is the same as defined above; R³ is hydrogen atom, etc.; X is halogen atom, etc., are reacted in the presence of a base, a copper catalyst and a palladium catalyst in an aprotic polar solvent.