Rilmenidine dihydrogen phosphate, S-3341, Hyperium, -Drug Synthesis Database

【结构式】

【药物名称】Rilmenidine dihydrogen phosphate, S-3341, Hyperium

【化学名称】2-(alpha,alpha-Dicyclopropylmethylamino)-2-oxazoline dihydrogen phosphate
　　　　　　2-(alpha,alpha-Dicyclopropylmethylamino)-4,5-dihydrooxazole dihydrogen phosphate
　　　　　　alpha,alpha-Dicyclopropyl-N-(4,5-dihydrooxazol-2-yl)methylamine dihydrogen phosphate
　　　　　　N-(Dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine dihydrogen phosphate

【CA登记号】54187-04-1, 54249-57-9 ((E)-2-butenedioate (1:1))

【分子式】C₁₀H₁₉N₂O₅P

【分子量】278.24713

【开发单位】Servier (Originator)

【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Imidazoline I1 Receptor Agonists

合成路线1

The addition of dicyclopropylmethylamine (II) to B-chloroethyl isocyanate (I) in THF gives N-(dicyclopropylmethyl)-N'-(Beta-chloroethyl)urea (III), which is then cyclized in refluxing water.

参考文献中间体

【1】 Malen, C.; Desnos, M.; Laubie, M.; Poignant, J.C. (Servier Laboratoires); Cyclopropylamines as pharmaceuticals. DE 2362754; ES 421879; FR 2212143; GB 1453703; JP 50004084; JP 53056664; JP 53056665 .
【2】 Castaner, J.; Prous, J.; S-3341. Drugs Fut 1986, 11, 6, 470.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	11237	1-Chloro-2-isocyanatoethane; 2-Chloroethyl isocyanate	1943-83-5	C₃H₄ClNO	详情	详情
(II)	24691	dicyclopropylmethanamine		C₇H₁₃N	详情	详情
(III)	24692	N-(chloromethyl)-N'-(dicyclopropylmethyl)urea		C₉H₁₅ClN₂O	详情	详情

Extended Information