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)
✍ Scribed by L. Pichat; J. P. Beaucourt; F. Krausz; C. Moulineau
- Publisher
- John Wiley and Sons
- Year
- 1976
- Tongue
- French
- Weight
- 409 KB
- Volume
- 12
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
Benzoyl chloride‐7^14^C 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‐^14^C) propionic acid. After cyclisation with hydrazine, followed by treatment with bromine in acetic acid, 3‐hydroxy‐4‐methyl‐6‐phenyl pyndazine 6‐^14^C is secured in a 77% yield. This hydroxypyridazine treated with POCl~3~ gave a 90% yield of 90 % pure 4‐methyl‐6‐phenyl‐3‐chloropyndazine 6‐^14^C; The latter treated with 2‐morpholino‐1‐aminoethane in presence of sodium iodide has given 3‐morpholinoethylamino 4‐methyl 6‐phenylpyndazine 6‐^14^C. The overall yield based on barium carbonate ^14^C is 16.7 % (specific activity 18.5 mCi/mMole).