Methods and intermediates for the synthesis of 3-aryl-3-hydroxy-phthalimidines.

摘要

This invention relates to new intermediates for the preparation of certain phthalimidines and phthalazinones. The intermediates are more particularly concerned with the preparation of 3-aryl-3-hydroxyphthalimidines which are useful as therapeutic agents. …The 3-aryl-3-hydroxyphthalimidines produced in accordance with the present invention are compounds of the formula: …… wherein,… Y and Z are each H, alkyl, halo alkoxy, trifluoromethyl, hydroxy, alkanoyloxy, or alkanoylamino;… X is F, Cl, Br or NR1R2 in which R1 and R2 are each hydrogen, alkyl, alkynyl, alkenyl, cycloalkyl, aryl or aralkyl; and… R is H, alkyl, cycloalkyl, or aralkyl.