PROCESS FOR PREPARING BENZOPYRAN DERIVATIVES

摘要

The cpd. of formula (I-a) is prepd. by (a) reacting ketone derivatives of formula (II) with trifluorosulfonic acid anhydride and ter-amine, or making the ketone derivatives (II) to enolate with a base and then reacting N-phenyl trifluoromethane sulfonimide to convert to the vinyl triflate derivs. of formula (III); and (b) reacting the derivs. (III) with pyridyl trialkyline derivs. of formula (IV) in the presence of palladium catalyst and chloride. In the formulas, R1 is -CN, -NO2, -OCX1X2X3, -NH2, -NHSO2Ra etc; X1, X2, and X3 are F, Cl or H; R3 is H or C1-6 alkyl or phenyl; R4 is C1-4 alkyl.