Synthesis Of 2,6-Dimethylbenzamide N-(5-Methyl-3-Isoxazolyl) (D2916) Labelled With C-14

Carbonation of 2,6-dimethyl phenyl lithium with (CO2)-C-14 afforded 2,6-dimethylbenzoic acid, alpha-C-14 2 which was transformed into 2,6-dimethylbenzoic acid halide, alpha-C-14 3. Subsequent condensation of the latter compound with 3-amino 5-methyl isoxazole afforded 2,6-dimethylbenzamide N-(5-methyl-3-isoxazolyl) (D2916)4 (radiochemical 95% purity) in an overall yield of about 35% based on [C-14] barium carbonate.