Synthese d'une pyridazine d'interet therapeutique, marquee au carbone 14: Dichlorhydrate de morpholinoethylamino-3 methyl-4 phenyl-6 pyridazine 14C-6 (30,038 CB)

Benzoyl chloride-714C is condensed with tris(trimethylsilyl) 1-lithio-1,1,2 propane tricarboxylate, which after hydrolysis gives rise to a 66% yield of 2-methyl-3-(benzoyl-7-14C) propionic acid. After cyclisation with hydrazine, followed by treatment with bromine in acetic acid, 3-hydroxy-4-methyl-6-phenyl pyndazine 6-14C is secured in a 77% yield. This hydroxypyridazine treated with POCl3 gave a 90% yield of 90 % pure 4-methyl-6-phenyl-3-chloropyndazine 6-14C; The latter treated with 2-morpholino-1-aminoethane in presence of sodium iodide has given 3-morpholinoethylamino 4-methyl 6-phenylpyndazine 6-14C. The overall yield based on barium carbonate 14C is 16.7 % (specific activity 18.5 mCi/mMole).