S-21407, EGIS-7229(fumarate salt), GYKI-16306

Chemical Name: 5-Chloro-4-[3-[N-[2-(3,4-dimethoxyphenyl)ethyl]-N-methylamino]propylamino]pyridazin-3(2H)-one
CAS No. 190333-92-7 (fumarate salt(1:1))
项目整合开发状态: Preclinical
项目研究机构: Egis (Originator), Institute for Drug Research (Originator), Servier (Licensee)
合成路线:Pyridazinone (I) was converted to 3,4,5-trichloropyridazine (VIII) on treatment with POCl3.Nucleophylic substitution in (II) with 3-aminopropanol (III) gave,after crystallization,the desired isomer (IV).Hydrolysis of the 3-chloro group of (IV) was carried out with AcOH and AcONa,resulting in the N,O-diacetyl derivative (V).Subsequent reaction of (V) with aqueous HBr provided bromide (VI),which was then treated with N-methyl homoveratrylamine (VII) to furnish the target compound (VIII).This compound was finally isolated as the fumarate salt on treatment with fumaric acid in EtOH (1).