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【结 构 式】 
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【药物名称】Colestilan, Colestimide, MCI-196, Cholebine 【化学名称】2-Methyl-1H-imidazole polymer with (chloromethyl oxirane) 【CA登记号】95522-45-5 【 分 子 式 】C7H11ClN2O 【 分 子 量 】174.63152 |
【开发单位】Mitsubishi Chemical (Originator), Mitsubishi Pharma (Originator), Yamanouchi (Comarketer), Mitsubishi Pharma (Codevelopment) 【药理作用】Lipoprotein Disorders, Treatment of , METABOLIC DRUGS, Renal Failure, Agents for, RENAL-UROLOGIC DRUGS, Treatment of Renal Diseases, Bile Acid Sequestrants, Cholesterol Absorption Inhibitors |
合成路线1
MCI-196 is synthesized by condensation of 2-methylimidazole (I) with epichlorohydrin (II) as follows: Equimolecular parts (0.5 M: 0.5 M) of (I) and (II) were allowed to condense in water (100 ml) at 90 C for 14 h; then 0.094 mol of (II) wa added and the reaction continued for 2 h at 45 C. The resulting resin was treated with 0.094 M of a 20% aqueous solution of NaOH and heated at 45 C for 2 h more. Finally, heat curing of the resin at 120 C for 5 h was performed. The resin was isolated by precipitation with water.
| 【1】 Toda, H. (Mitsubishi Chemical Corp.); Process for the preparation of granular basic ion exchange resins. JP 1985245626 . |
| 【2】 Nomura, T.; Hamada, Y.; Kurihara, Y. (Mitsubishi Chemical Corp.); Oral hypocholesterolemic agents. JP 1992013627 . |
| 【3】 Nomura, T.; Hamada, Y.; Kurihara, Y. (Mitsubishi Chemical Corp.); Oral hypocholesterolemic agents. JP 1990124819 . |
| 【4】 Toda, H.; Kihara, K. (Bristol-Myers Squibb Co.); Novel quaternary salt of polymer. BE 0898807; CH 663415; DE 3403125; GB 2134119; NL 8400237 . |
| 【5】 Toda, H.; Kihara, K. (Mitsubishi Chemical Corp.); Improved preparation process for anion exchange resins. JP 1984155421 . |
| 【6】 Toda, H.; Mizogami, S.; Kihara, K.; Hashimoto, M.; Bile acid binding and hypocholesterolemic activity of a new anion exchange resin from 2-methylimidazol and epichlorohydrin. J Pharm Sci 1988, 77, 6, 531. |
| 【7】 Castaner, J.; Prous, J.; MCI-196. Drugs Fut 1993, 18, 1, 15. |