Carvedilol, SK&F-105517, DQ-2466, BM-14190, Coreg CR, Querto, Dibloc, Coropress, Eucardic, Coreg, Artist, Dimitone, Dilatrend, Kredex

合成路线:By condensation of 4-(2,3-epoxypropoxy)carbazole (I) with 2-(2-methoxyphenoxy)ethylamine (II) at 70 C in diglime.

参考文献标题:Carvedilol
文献作者:Aronhime,J.; Dolitzky,B.-Z.; Finogueev,S.; Kor,I.; Ben-Valid,S.; Hildesheim,J.(Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA,Inc.)
参考来源:WO 0200216


合成路线:This compound has been obtained in two related ways:1.The reaction of 2-(2-bromoethoxy)anisole (I) with benzylamine (II) by heating at 80 C gives the secondary amine (III),which is condensed with epichlorohydrin (IV) by heating at 60 C to yield the isopropanol derivative (V).The condensation of (V) with 4-hydroxycarbazole (VI) by means of K2CO3 in refluxing dioxane affords the adduct (VII),which is finally debenzylated by hydrogenolysis with H2 over Pd/C in ethanol/water.2.The condensation of the secondary amine (III) with 4-(2,3-epoxypropoxy)carbazole (VIII) in refluxing ethanol gives the already reported adduct (VII),which is debenzylated as indicated.

参考文献标题:Process and intermediates for preparing 1-[9'H-carbazol-4'-yloxy]-3-[2''-(2'''-methoxy-phenoxy)ethyl]amino]-propan-2-ol (carvedilol)
文献作者:Seres,P.; Cselenyak,J.; Nagy,K.; Simig,G.; Gregor,T.; Nagy,P.K.; Greff,Z.; Balazs,L.; Barkoczy,J.; Vereczkey,G.D.; Nemeth,N.; Szabo,T.; Ratkai,Z.; Doman,I.(Egis Pharmaceuticals Ltd.)
参考来源:EP 0918055


合成路线:By condensation of 4-(2,3-epoxypropoxy)carbazole (I) with 2-(2-methoxyphenoxy)ethylamine (II) at 70 C in diglime.
参考文献标题:BM-14,190
文献作者:Grau,M.; Serradell,M.N.; Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1983,8(10),841


产品链接: CAS No. 72956-09-3››