Flezelastine is a new phthalazinone derivative with antiasthmatic/anti
allergic activity. For pharmacokinetic studies C-14-labeled flezelasti
ne was synthesized starting with [7,8-C-14]-phthalic anhydride. In a c
onvergent synthesis 1.5 g of double C-14-labeled flezelastine hydrochl
oride (ASTA code: D-18024) with a specific activity of 3 MBq/mg was ob
tained.