Etacizin, Ethacizin, NIK-244
N-[10-(3-二乙基氨基丙酰基)吩噻嗪-2-基]氨基甲酸乙酯Chemical Name: 2-(Ethoxycarbonylamino)-10-[3-(diethylamino)propionyl]phenothiazine; [10-[3-(Diethylamino)-1-oxopropyl]-10H-phenothiazin-2-yl]carbamic acid ethyl ester
CAS No. 33414-33-4
项目整合开发状态: Launched-1989
项目研究机构: Nauchno-Issledovatelsky Institut (Originator), Nikken Chemicals (Originator)
合成路线:By reaction of 10-(3-chloropropionyl)-2-(ethoxycarbonylamino)phenothiazine (I) with diethylamine in refluxing toluene.
📌 参考资料/链接：
参考文献标题:Agent for treating myocardial infarction
文献作者:Cazov,E.I.; Valdman,A.V.; Kaverine,N.V.; Penke,I.C.; Rozenstrauch,L.V.; Cicharev,V.N.; Prjanisnikova,N.T.; Senota,Z.P.; Lyskovcev,V.V.; Grigorieva,E.K.; Skoldinov,A.P.; Gricenko,A.N.; Ermakova,Z.I.; et al.(Nauchno-Issledovatelsky Institut)
参考来源:DE 3314142
📄 详细内容
合成路线:By reaction of 10-(3-chloropropionyl)-2-(ethoxycarbonylamino)phenothiazine (I) with diethylamine in refluxing toluene.
合成路线:This compound can be obtained in two different ways:1) The bromination of 1-(2-ethylindan-2-yl)-1-ethanone (I) with Br2 in ether gives 2-bromo-1-(2-ethylindan-2-yl)-1-ethanone (II),which is then cyclized with formamide by heating at 170-80 C.2) The cyclization of alpha,alpha'-dibromo-o-xylene (III) with 4-penten-2-one (IV) by means of tetrabutylammonium hydroxide in toluene at 100 C gives 1-(2-vinylindan-2-yl)-1-ethanone (V),which is brominated with Br2 in dichloromethane to yield 2-bromo-1-(2-vinylindan-2-yl)-1-ethanone (VI).The cyclization of (VI) with formamide at 160 C as before affords 4-(2-vinylindan-2-yl)-1H-imidazole (VII),which is finally hydrogenated with H2 over Pd/C in ethanol.
参考文献标题:4(5)-Substd.imidazole derivs.,and intermediates and processes for their preparation
文献作者:Karjalainen,A.L.; Karjalainen,A.J.(Orion Pharma)
参考来源:EP 0247764; US 4933359
合成路线:By reaction of 10-(3-chloropropionyl)-2-(ethoxycarbonylamino)phenothiazine (I) with diethylamine in refluxing toluene.
参考文献标题:ETHACIZIN
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1990,15(1),28
产品链接: CAS No. 33414-33-4››