药物详细合成路线

Name	Sofalcone
Chemical Name	2-[5-(3-Methyl-2-butenyloxy)-2-[3-[4-(3-methyl-2-butenyloxy)phenyl]-2(E)-propenoyl]phenoxy]acetic acid
CAS	64506-49-6
Related CAS
Formula	C27H30O6
Structure
Formula Weight	450.53655
Stage	临床前
Company	Taisho (Originator)
Activity/Mechanism	Antiulcer Drugs, GASTROINTESTINAL DRUGS
Syn. Route	1

Route 1 the reaction of 2-hydroxy-4-(3-methyl-2-butenyloxy)acetophenone (i) with ethyl bromoacetate (ii) by means of koh in acetone gives 2-ethoxycarbonylmethoxy-4-(3-methyl-2-butenyloxy)acetophenone (iii), which is then condensed with 4-(3-methyl-2-butenyloxy)benzaldehyde (iv) by means of koh in ethanol. List of intermediates No. methyl 1-hydrazinecarbimidothioate (i) [(2r,3s,4s,5r)-5-(6-amino-2-fluoro-9h-purin-9-yl)-3,4-dihydroxytetrahydro-2-furanyl]methyl diethyl phosphate (ii) bromo[4-[(triisopropylsilyl)oxy]phenyl]magnesium (iv) n-[(1r,2r)-2-aminocyclohexyl]-n-tritylamine; (1r,2r)-n(1)-trityl-1,2-cyclohexanediamine (iii) Reference 1:     grau, m.; castaner, j.; blancafort, p.; serradell, m.n.; su-88. drugs fut 1983, 8, 6, 513. Reference 2:     kyogoku, k.; hatayama, k.; yokomori, s.; sawada, j.; tanaka, i. (taisho pharmaceutical co., ltd.); 2-(carboxymethoxy)chalcones. de 2705603; es 455620; fr 2340924; gb 1523241; jp 52097950; us 4085135 .

来源:药化网

作者:药化小编

摘要:本文合成路线介绍的是药物中文名索法酮；英文名Sofalcone；CAS[64506-49-6]

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