Degradation products of ketoconazole

Abstract

Photolysis of ketoconazole in four organic solvents with free access to air studied. It is found that the degradation products occurred when using methanol as solvent and with the optimum UV irradiation duration of 15 hours give better yields than acetone, ethylacetate and chloroform in the same condition. The isolated degradation products is 1-acetyl-4-[4-[[(lH-imidazo [2,1-a]3,4-dihydro-7-chloro-isoquinolyl)-6-spiro-2' -(1,3 -dioxolan-4-yl)] methoxy]phenyl]piperazine. The structure was elucidated by spectro copic techniques. Photolytic reaction mechanism is proposed via free radical and cyclization.