藥物詳細合成路線

Name	Rilmenidine dihydrogen phosphate;S-3341;Hyperium
Chemical Name	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
CAS	54187-04-1
Related CAS	54249-57-9 ((E)-2-butenedioate (1:1))
Formula	C10H19N2O5P
Structure
Formula Weight	278.24713
Stage	上市-1988
Company	Servier (Originator)
Activity/Mechanism	CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Imidazoline I1 Receptor Agonists
Syn. Route	1

Route 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. List of intermediates No. benzhydryl 2-(aminooxy)-2-[3,4-bis(acetoxy)phenyl]acetate (i) methyl 5-[(3ar,4r,5r,6as)-5-(acetoxy)-4-[(e,3s,4r)-3-(acetoxy)-4-methyl-1-octenyl]hexahydro-2h-cyclopenta[b]furan-2-yl]-5-iodopentanoate (ii) methyl 5-[(3ar,4r,5r,6as)-5-(acetoxy)-4-[(e,3s,4s)-3-(acetoxy)-4-methyl-1-octenyl]hexahydro-2h-cyclopenta[b]furan-2-ylidene]pentanoate (iii) Reference 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 . Reference 2:     castaner, j.; prous, j.; s-3341. drugs fut 1986, 11, 6, 470.

來源:藥化網

作者:藥化小編

摘要:本文合成路線介紹的是藥物中文名利美尼啶；英文名Rilmenidine dihydrogen phosphate;S-3341;Hyperium；CAS[54187-04-1]

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