甲 唑-[CAS443-48-1]-合成路线图解——原料药厂家武汉东康源2.doc

最新精品文档，知识共享！ 药物详细合成路线 Name Metronidazole;IDR-90105(Ophthalmic);Rosased;Zidoval;Metrogel;Flagyl Chemical Name 2-Methyl-5-nitro-1H-imidazole-1-ethanol CAS 443-48-1 Related CAS 133884-00-1 (deleted CAS) Formula C6H9N3O3 Structure Formula Weight 171.15693 Tel E-mail 027 袁经理 chem@ Company 武汉东康源科技有限公司 Activity/Mechanism Acne Therapy, Antiamebics, Antibacterial Drugs, Antibacterial Ophthalmic Drugs, Antifungal Agents, ANTIINFECTIVE THERAPY, Antitrichomonals, DERMATOLOGIC DRUGS, Ocular Antiinflammatory and Antiinfective Agents, OCULAR MEDICATIONS, Ophthalmic Drugs, Treatment of Protozoal Diseases Syn. Route 6 Route 1 2-methylimidazole (i) is converted into the bisulfate salt, and then nitrated by means of a sulfonitric mixture in ac2o to produce 2-methyl-4-nitroimidazole (ii) . in a variant of this procedure, 2-methylimidazole (i) is nitrated by using a ferric nitrate-tonsyl adduct in several solvents. imidazole (ii) is then regioselectively alkylated with boiling 2-chloroethanol to produce the title compound. alternatively, the alkylation of (ii) has been reported by treatment with ethylene oxide (iii) under acidic conditions. Route 2 in an alternative procedure, the title compound is obtained by hydrolysis of the bromoethyl imidazole (i) in the presence of formic acid in aqueous formamide List of intermediates No. Reference 1: sunjic, v.; fajdiga, t.; kajfez, f.; process for preparation of 1-(2-hydroxyethyl)-2-methyl-5-nitroimidazole. de 1695321; gb 1138805; us 3520900 . Route 3 the title compound can be obtained by reaction of 1-(acetoxymethyl)-2-methyl-4-nitroimidazole (i) with ethylene oxide (ii) in the presence of sulfur trioxide, followed by hydrolysis in aqueous h2so4 List of intermediates No. 3-(4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl)-4-phenyl-1,4-dihydropyridine (ii) Reference 1: lavigne, m.; mandard-cazin, b. (aventis pharma sa); process for preparing hydroxyalkyl-1 nitro-5 imidazoles. wo 9113877 . Route 4 in a related procedure