Dazmegrel, UK-38485

达美格雷Chemical Name: 3-(1H-Imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid; 1-(2-Carboxyethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole
CAS No. 76894-77-4
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator)
合成路线:The condensation of 2-methyl-3-(1H-imidazol-1-ylmethyl)indole (III) with acrylonitrile (IV) by means of benzyltrimethylammonium hydroxide (B) in dioxane gives 1-(2-cyanoethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole (V),which is then hydrolyzed with KOH in water.The reaction of compound (III) with methyl acrylate (VI) in the same conditions as before gives 1-(2-methoxy-carbonylethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole (VII),which is also hydrolyzed.Compound (III) can be obtained from 2-methylindole (I).
📌 参考资料/链接:
参考文献标题:Inhibition of thromboxane synthetase by 3-(1-imidazolylalkyl)indoles
文献作者:Cross,P.E.; Dickinson,R.P.(Pfizer Inc.)
参考来源:NL 8001351

📄 详细内容


合成路线:The condensation of 2-methyl-3-(1H-imidazol-1-ylmethyl)indole (III) with acrylonitrile (IV) by means of benzyltrimethylammonium hydroxide (B) in dioxane gives 1-(2-cyanoethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole (V),which is then hydrolyzed with KOH in water.The reaction of compound (III) with methyl acrylate (VI) in the same conditions as before gives 1-(2-methoxy-carbonylethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole (VII),which is also hydrolyzed.Compound (III) can be obtained from 2-methylindole (I).

参考文献标题:UK-38485
文献作者:Serradell,M.N.; Castar,J.; Blancafort,P.; Grau,M.
参考来源:Drugs Fut 1983,8(11),947


合成路线:The condensation of 2-methyl-3-(1H-imidazol-1-ylmethyl)indole (III) with acrylonitrile (IV) by means of benzyltrimethylammonium hydroxide (B) in dioxane gives 1-(2-cyanoethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole (V),which is then hydrolyzed with KOH in water.The reaction of compound (III) with methyl acrylate (VI) in the same conditions as before gives 1-(2-methoxy-carbonylethyl)-2-methyl-3-(1H-imidazol-1-ylmethyl)indole (VII),which is also hydrolyzed.Compound (III) can be obtained from 2-methylindole (I).
参考文献标题:K-38485,a novel,selective thromboxane synthetase inhibitor with prolonged activity in vivo
文献作者:Cross,P.E.; Dickinson,R.P.; Randall,M.J.; Parry,M.J.
参考来源:N Am Med Chem Symp 1982,68


产品链接: CAS No. 76894-77-4››