Fluorination process of anilide derivatives and benzothiazole fluorinate derivatives as in vivo imaging agents

摘要

Disclosed is a process for preparation of a fluoroanilide of formula (I): wherein R1 is selected from alkyl, alkenyl, and alkynyl; which comprises: (i) reaction of a corresponding arylamide of formula (II): wherein R2 is selected from hydrogen, alkyl, haloalkyl, aryl, arylalkyl, -(CH2CH2O)q-CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group; with fluoride to give a compound of formula (III) wherein R1 and R2 are as defined for the compound of formula (I); followed by step (ii) where step (ii) is conversion of group -C(O)R2 to hydrogen. Also disclosed is a compound of formula (IIa) or (IIb) in particular 2-[3-nitro-4-(methylformylamino)phenyl]-6-ethoxymethoxy-benzothiazole.