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Minoxidil, TM-160, U-10858, Minoximen, Neoxidil, RiUP, Loniten, Rogaine, Regaine

米诺地尔Chemical Name: 6-Amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine
CAS No. 38304-91-5
项目整合开发状态: Launched-1980
项目研究机构: Pfizer (Originator), Menarini (Licensee), Taisho (Licensee)
合成路线:Compound can be prepared in tvvo different ways both starting from 2,4-diamino-6-chloropyrimidine (I):1) The oxidation of (I) with m-chloroperbenzoic acid in alcohol gives 6-amino-4-chloro-1,2-dihydro-1-hydroxy-2-iminopyrimidine (II),which is then condensed with refluxing piperidine.2) A mixture of (I),2,4-dichlorophenol (A) and KOH was heated at 150 C to give 2,4-diamino-6-(2,4-dichlorophenoxy)pyrimidine (III),which is oxidized with m-chloroperbenzoic acid in alcohol giving 6-amino-4-(2,4-dichlorophenoxy)-1,2-dihydro-1-hydroxy-2-iminopyrimidine (IV).Finally,this product is treated with piperidine at 150 C.
📌 参考资料/链接:
参考文献标题:Minoxidil
文献作者:Castar,J.; Sungurbey,J.
参考来源:Drugs Fut 1977,2(6),383

📄 详细内容


合成路线:Compound can be prepared in tvvo different ways both starting from 2,4-diamino-6-chloropyrimidine (I):1) The oxidation of (I) with m-chloroperbenzoic acid in alcohol gives 6-amino-4-chloro-1,2-dihydro-1-hydroxy-2-iminopyrimidine (II),which is then condensed with refluxing piperidine.2) A mixture of (I),2,4-dichlorophenol (A) and KOH was heated at 150 C to give 2,4-diamino-6-(2,4-dichlorophenoxy)pyrimidine (III),which is oxidized with m-chloroperbenzoic acid in alcohol giving 6-amino-4-(2,4-dichlorophenoxy)-1,2-dihydro-1-hydroxy-2-iminopyrimidine (IV).Finally,this product is treated with piperidine at 150 C.

参考文献标题:N-Alkyl pyrrolidone-plasticized copolylactam compositions
文献作者:Hyde,T.J.
参考来源:US 3644264


合成路线:Compound can be prepared in tvvo different ways both starting from 2,4-diamino-6-chloropyrimidine (I):1) The oxidation of (I) with m-chloroperbenzoic acid in alcohol gives 6-amino-4-chloro-1,2-dihydro-1-hydroxy-2-iminopyrimidine (II),which is then condensed with refluxing piperidine.2) A mixture of (I),2,4-dichlorophenol (A) and KOH was heated at 150 C to give 2,4-diamino-6-(2,4-dichlorophenoxy)pyrimidine (III),which is oxidized with m-chloroperbenzoic acid in alcohol giving 6-amino-4-(2,4-dichlorophenoxy)-1,2-dihydro-1-hydroxy-2-iminopyrimidine (IV).Finally,this product is treated with piperidine at 150 C.
参考文献标题:6-Amino-1,2-dihydro-1-hydroxy-2-imino-4-phenoxypyrimidines
文献作者:Anthony,W.C.; et al.
参考来源:CH 495361; DE 1795837; FR 1510017; GB 1167736; US 3382247; US 3382248; US 3461461


产品链接: CAS No. 38304-91-5››