PROCESS FOR PRODUCING SUBSTITUTED GEMINAL DIHALOGENO-DERIVATIVES OF PYRIDO-SQUARE BRACKET-1,2-A-SQUARE CLOSED-PYRIMIDINES,PYRROLO-SQUARE BRACKET-1,2-A-SQUARE BRACKET CLOSED-PYRIMIDINES AND PYRIMIDO-SQUARE BRACKET-1,2,-A-SQUARE BRACKET CLOSED-ASEPINES

摘要

Geminal dihalogen derivatives of condensed pyrimidine-4-one compounds of the general formula IMAGE [wherein R represents hydrogen, lower alkyl, or lower alkoxycarbonyl; R1 represents hydrogen, lower alkyl, ester group, carboxy or a derivative thereof, cyano, phenyl or halogen; R2 represents hydrogen, lower alkyl or phenyl; X represents halogen; n is the integer 0, 1 or 2] and the salts and optically active antipodes thereof are of interest as chemical intermediates; some also exhibit a variety of physiological activities and may be formulated into pharmaceutical compositions in conventional manner. The novel compounds can be made by halogenating a corresponding starting material wherein one or both X-substituents are hydrogen.