Synthesis of tritium-labelled 2-(3′-carboxypropyl)-3-imino-6 para-methoxy phenyl-2,3-dihydropyridazine ([3H] SR95531)

✍ Scribed by A. Melikian Gh; G. Schlewer; S. Hurt; D. Chantreux; C. C. Wermuth

• Publisher: John Wiley and Sons
• Year: 1987
• Tongue: French
• Weight: 270 KB
• Volume: 24
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580240306

✦ Synopsis

The synthesis o f t r i t i u m l a b e l l e d 2 -(3'-carboxypropyl)-3-imino-6para-methoxyphenyl-2,3-dihydropyridazine, a new, s p e c i f i c , waters o l u b l e and chemically s t a b l e GABA antagonist a t t h e GABAA r e c e p t o r s i t e i s reported. The synthesis i n v o l v e s an N-2 e n d o -a l k y l a t i o n o f 3-amino-6-p-methoxyphenyl-pyridazine w i t h e t h y l y-bromocrotonate, r e d u c t i v e t r i t i a t i o n o f t h e c r o t o n i c double bond and h y d r o l y s i s i n a c i d i c medium.