Mopidralazine, MDL-899
莫哌屈嗪Chemical Name: N-(2,5-Dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine; 4-[6-[(2,5-Dimethylpyrrol-1-yl)amino]-3-pyridazinyl]morpholine
CAS No. 75841-82-6, 75841-84-8 (HCl), 77510-09-9 (sulfate)
项目整合开发状态: Biological Testing
项目研究机构: Lepetit (Originator)
合成路线:The starting compound is 3,6-dichloropyridazine (I),which is reacted with morpholine (II) in a suitable solvent to give 3-morpholino-6-chloropyridazine (III).This,upon reaction with hydrazine hydrate as solvent,gives the hydrazine derivative (IV),which by reaction with acetonylacetone (V) in acetic acid yields directly the title compound.[14C]-Labeled compound is synthesized by a microscale procedure with 45% chemical yield and 98% radiochemical purity.
📌 参考资料/链接：
参考文献标题:Mopidralazine
文献作者:Koch,H.
参考来源:Drugs Fut 1985,10(8),634
📄 详细内容
合成路线:The starting compound is 3,6-dichloropyridazine (I),which is reacted with morpholine (II) in a suitable solvent to give 3-morpholino-6-chloropyridazine (III).This,upon reaction with hydrazine hydrate as solvent,gives the hydrazine derivative (IV),which by reaction with acetonylacetone (V) in acetic acid yields directly the title compound.[14C]-Labeled compound is synthesized by a microscale procedure with 45% chemical yield and 98% radiochemical purity.
合成路线:The cyclization of methyl acetoacetate (I),2-methoxybenzaldehyde (II) and thiourea (III) by means of HCl in refluxing ethanol gives the tetrahydropyrimidine (IV),which is finally cyclized with chloroacetic acid (V) and benzaldehyde (VI) by means of sodium acetate in a refluxing mixture of acetic acid and acetic anhydride.
参考文献标题:Pharmacokinetics of a new antihypertensive pyrrolyl pyridazinamine (MDL-899) in the rat and the dog
文献作者:Assandri,A.; et al.
参考来源:Arzneim-Forsch Drug Res 1985,35(2),508
产品链接: CAS No. 75841-82-6››