Alizapride, Limican, Liticum
阿立必利Chemical Name: 5-(1-Allylpyrrolidin-2-ylmethylaminocarbonyl)-6-methoxybenzotriazole
CAS No. 59338-93-1
项目整合开发状态: Launched-1981
项目研究机构: Delagrange (Originator), Sanofi-Aventis (Originator)
合成路线:The nitration of methyl 2-methoxy-4-aminobenzoate (I) with nitric acid in acetic acid-acetic anhydride,followed by hydrolysis with methanolic H2SO4 gives methyl 2-methoxy-4-amino-5-nitrobenzoate (II),which is reduced with H2 over Raney-Ni in methanol to yield methyl-2-methoxy-4,5-diaminohenzoate (III).The cyclization of (III) with NaNO2 in aqueous HCl affords methyl 6-methoxybenzotriazole-5-carboxylate (IV),which is finally condensed with 1-allylpyrrolidin-2-ylmethylamine (V) in refluxing toluene.
📌 参考资料/链接：
参考文献标题:N-(1'-allypyrrolidinyl-2'-methyl)-2-methoxy-4,5-azimido benzamide and its pharmaceutically acceptable salts
文献作者:Bulteau,G.; Acher,J.; Collignon,C.; Monier,J.-C.(Societe d'Etudes Scientifiques et Industrielles de L'Ile de France)
参考来源:US 4039672
📄 详细内容
合成路线:The nitration of methyl 2-methoxy-4-aminobenzoate (I) with nitric acid in acetic acid-acetic anhydride,followed by hydrolysis with methanolic H2SO4 gives methyl 2-methoxy-4-amino-5-nitrobenzoate (II),which is reduced with H2 over Raney-Ni in methanol to yield methyl-2-methoxy-4,5-diaminohenzoate (III).The cyclization of (III) with NaNO2 in aqueous HCl affords methyl 6-methoxybenzotriazole-5-carboxylate (IV),which is finally condensed with 1-allylpyrrolidin-2-ylmethylamine (V) in refluxing toluene.
参考文献标题:Alizapride
文献作者:Leeson,P.A.; Serradell,M.N.; Castar,J.; Blancafort,P.; Mealy,N.E.
参考来源:Drugs Fut 1981,6(1),11
产品链接: CAS No. 59338-93-1››