新产品编号:1256617
Chemical Name: 5-(2-Methoxyphenyl)-7-methyl-3-oxo-2(Z)-benzylidene-5H-1,3-thiazolo[3,2-a]pyrimidine-6(3H)-carboxylic acid methyl ester
项目整合开发状态: Preclinical
项目研究机构: Hacettepe University (Originator), Westf鋖ische Wilhelms-Univ. M黱ster (Originator)
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.
📌 参考资料/链接：
参考文献标题:Condensed heterocyclic compounds: Synthesis and antiinflammatory activity of novel thiazolo[3,2-a]pyrimidines
文献作者:Kelicen,P.; Ertan,M.; Demirdamar,R.; Krebs,B.; Tozkoparan,B.; L鋑e,M.
参考来源:Arch Pharm 1998,331(6),201
📄 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