新产品编号:1721725
Chemical Name: 4-Acetyl-[7-[3-(3,4-dimethoxybenzylamino)-2-hydroxypropoxy]-3,4-dihydro-2H-1,4-benzoxazine
项目整合开发状态: Preclinical
项目研究机构: Otsuka (Originator)
合成路线:The acylation of 7-hydroxy-3,4-dihydro-2H-1,4-benzoxazine (I) with acetic anhydride gives the N-acetyl derivative (II),which is condensed with epichlorohydrin (III) by means of K2CO3 at 90-5 C yielding 4-acetyl-7-(2,3-epoxypropoxy)-3,4-dihydro-2H-1,4-benzoxazine (IV).Finally,the addition of 3,4-dimethoxybenzylamine (V) to the epoxy group of (IV) in hot isopropanol affords the target compound.
📌 参考资料/链接:
参考文献标题:Synthesis of oxypropanolamine derivatives of 3,4-dihydro-2H-1,4-benzoxazine,beta-adrenergic affinity,inotropic,chronotropic and coronary vasodilating activities
文献作者:Iakovou,K.; Kazanis,M.; Vavayannis,A.; Bruni,G.; Romeo,M.R.; Massarelli,P.; Teramoto,S.; Fujiki,H.; Mori,T.
参考来源:Eur J Med Chem 1999,34(11),903