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

2006 
A process for preparing a compound of formula (I): ** ** Formula wherein the phenyl ring is optionally substituted with 1 to 4 substituents; R1 is selected from C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl; comprising: (i) reacting a corresponding compound of formula (II): Formula ** ** wherein ring A is optionally substituted as defined for compound of formula (I); R2 is selected from hydrogen, C1-10 alkyl, C1-10 haloalkyl, C6-14 aryl, aryl (C6-14) -alkyl, - (CH2CH2O) q-CH3 wherein q is an integer from 1 to 10; R1 is as defined for compound of formula (I); and R3 is a leaving group; with fluoride to give a compound of formula (III), whereby said leaving group is displaced by reaction with fluoride such ** ** Formula wherein R1 and R2 are as defined for compound of formula (I) and the ring phenyl a is substituted as defined for compound of formula (I); followed by step (ii) and optionally step (iii) in any order (ii) conversion of group -C (O) R2 hydrogen, suitably by hydrolysis (iii) removal of any protecting group more.
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