Esmolol hydrochloride, ASL-8052, Brevibloc
艾司洛尔Chemical Name: (?-3-[4-[2-Hydroxy-3-(isopropylamino)propoxy]phenyl]propionic acid methyl ester hydrochloride; (?-Methyl p-[2-hydroxy-3-(isopropylamino)propoxy]hydrocinnamate hydrochloride
CAS No. 84057-94-3 ((+)-enantiomer, free base), 103598-03-4 (free base), 81147-92-4 (free base, non-specified stereoch.), 81161-17-3 (undefined stereoch.)
项目整合开发状态: Launched-1987
项目研究机构: Bristol-Myers Squibb (Originator), Sigma-Tau (Not Determined), Almirall Prodesfarma (Licensee), Baxter (Licensee)
合成路线:The esterification of 3-(4-hydroxyphenyl)propionic acid (I) with methanol and H2SO4 gives the corresponding methyl ester (II),which by condensation with epichlorohydrin (III) by means of K2CO3 in refluxing acetone affords methyl 3-[4-(2,3-epoxypropoxy)phenyl]propionate (IV).Finally,the epoxide ring is opened by reaction with isopropylamine (V) in refluxing methanol,and a final treatment with ethereal HCl is performed.
📌 参考资料/链接：
参考文献标题:Method for treatment or prophylaxis of cardiac disorders
文献作者:Erhardt,P.W.; Bogman,R.J.; O'Donnell,J.P.(Baxter International Inc.)
参考来源:EP 0053435; EP 0065542; US 4387103; WO 8201869
📄 详细内容
合成路线:The esterification of 3-(4-hydroxyphenyl)propionic acid (I) with methanol and H2SO4 gives the corresponding methyl ester (II),which by condensation with epichlorohydrin (III) by means of K2CO3 in refluxing acetone affords methyl 3-[4-(2,3-epoxypropoxy)phenyl]propionate (IV).Finally,the epoxide ring is opened by reaction with isopropylamine (V) in refluxing methanol,and a final treatment with ethereal HCl is performed.
参考文献标题:Esmolol Hydrochloride
文献作者:Serradell,M.N.; Castar,J.; Bad韆,A.
参考来源:Drugs Fut 1984,9(3),183
合成路线:The esterification of 3-(4-hydroxyphenyl)propionic acid (I) with methanol and H2SO4 gives the corresponding methyl ester (II),which by condensation with epichlorohydrin (III) by means of K2CO3 in refluxing acetone affords methyl 3-[4-(2,3-epoxypropoxy)phenyl]propionate (IV).Finally,the epoxide ring is opened by reaction with isopropylamine (V) in refluxing methanol,and a final treatment with ethereal HCl is performed.
参考文献标题:Ultra-short-acting beta-adrenergic receptor blocking agents.2.(Aryloxy)propanolamines containing esters on the aryl function
文献作者:Erhardt,P.W.; Woo,C.M.; Anderson,W.G.; Gorczynski,R.J.
参考来源:J Med Chem 1982,25(12),1408
产品链接: CAS No. 84057-94-3›› 产品链接: CAS No.103598-03-4››