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【结 构 式】 
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【药物名称】ME-3221 【化学名称】3-Methoxy-2,6-dimethyl-4-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethoxy]pyridine 【CA登记号】139958-16-0 【 分 子 式 】C22H21N5O2 【 分 子 量 】387.44497 |
【开发单位】Meiji Seika (Originator) 【药理作用】CARDIOVASCULAR DRUGS, Hypertension, Treatment of, Angiotensin AT1 Antagonists |
合成路线1
The condensation of 3-methoxy-2,6-dimethylpyridin-4(1H)-one (I) with 5-[4'-(bromomethyl)biphenyl-2-yl]-1-(triphenylmethyl)tetrazole (II) by means of NaH in hot DMF gives the condensation product (III), which is finally deprotected by treatment with HCl in methanol/dichloromethane.
| 【1】 Mealy, N.; Ngo, J.; Castaner, J.; ME-3221. Drugs Fut 1996, 21, 8, 794. |
| 【2】 Katano, K.; Ogino, H.; Shitara, E.; Watanabe, H.; Nagura, J.; Osada, N.; Ichimaru, Y.; Konno, F.; Machinami, T.; Tsuruoka, T. (Meiji Seika Kaisha, Ltd.); Pyridine derivs. with angiotensin II antagonism. EP 0487745; US 5399566; WO 9119697 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 15908 | 3-methoxy-2,6-dimethyl-4(1H)-pyridinone | C8H11NO2 | 详情 | 详情 | |
| (II) | 15538 | 5-[4'-(bromomethyl)[1,1'-biphenyl]-2-yl]-2-trityl-2H-1,2,3,4-tetraazole | 124750-51-2 | C33H25BrN4 | 详情 | 详情 |
| (III) | 15910 | 2,6-dimethyl-4-[[2'-(1-trityl-1H-1,2,3,4-tetraazol-5-yl)[1,1'-biphenyl]-4-yl]methoxy]-3-pyridinyl methyl ether; 3-methoxy-2,6-dimethyl-4-[[2'-(1-trityl-1H-1,2,3,4-tetraazol-5-yl)[1,1'-biphenyl]-4-yl]methoxy]pyridine | C41H35N5O2 | 详情 | 详情 |
Extended Information