trans-4-amino-3,4-dihydro-2,2-dimethyl-6-trifluoromethylsulfonyl 2H-1-benzopyran-3-ol → trans-4-(4-Fluoro-1-oxoisoindolin-2-yl)-3,4-dihydro-2,2-dimethyl-6-trifluoromethylsulfonyl-2H-1-benzopyran-3-ol

Participants

Reaction Steps

Following the procedure and working up described in Example 12, but using 0.272 g of methyl 2-bromomethyl-3-fluorobenzoate, 0.326 g of trans-4-amino-3,4-dihydro-2,2-dimethyl 6-trifluoromethylsulfonyl-2H-1-benzopyran- 3-ol and 0.15 ml of triethylamine, 0.294 g of the title compound, melting at 259°-261° C., was obtained after purification by column chromatography through silica gel, using a 1:1 by volume mixture of cyclohexane and ethyl acetate as the eluent, followed by recrystallization from a mixture of ethyl acetate and hexane.

Provenance & Evidence