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【结 构 式】 
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【分子编号】25075 【品名】2-methoxy-3-pyridinamine 【CA登记号】 |
【 分 子 式 】C6H8N2O 【 分 子 量 】124.1424 【元素组成】C 58.05% H 6.5% N 22.57% O 12.89% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(I)The condensation of 2-methoxypyridine-3-amine (I) with ethyl 2-(ethoxymethylene)-3-oxohexanoate (II) by heating at 120-30 C gives the aminoacrylate ewster (III), which is cyclized by heating in refluxing diphenyl ether to yield the naphthyridinone (IV). The reaction of (IV) with methanesulfonyl chloride and triethylamine in dichloromethane affords the methanesulfonyloxy naphthyridine (V), which is finally condensed with (R)-1-phenylethylamine (VI) in refluxing acetonitrile.
| 【1】 Sohn, S.K.; Chang, M.S.; Kim, S.G.; Chung, K.J.; Kang, D.P.; Kim, Y.H.; Kang, B.G.; Choi, W.S.; Seo, K.H.; Yoo, H.Y.; Paek, J.H. (Yung-Jin Pharmaceutical Co., Ltd.); 4-Amino-3-acylnaphthyridine derivs.. WO 9703074 . |
| 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) | 25075 | 2-methoxy-3-pyridinamine | C6H8N2O | 详情 | 详情 | |
| (II) | 12517 | ethyl (E)-2-butyryl-3-ethoxy-2-propenoate | C11H18O4 | 详情 | 详情 | |
| (III) | 25076 | ethyl (Z)-2-butyryl-3-[(2-methoxy-3-pyridinyl)amino]-2-propenoate | C15H20N2O4 | 详情 | 详情 | |
| (IV) | 25077 | 3-butyryl-8-methoxy[1,7]naphthyridin-4(1H)-one | C13H14N2O3 | 详情 | 详情 | |
| (V) | 25078 | 8-methoxy-4-[[methyl(dimethylene)-lambda(6)-sulfanyl]oxy]-3-(1-propylvinyl)[1,7]naphthyridine | C17H22N2O2S | 详情 | 详情 | |
| (VI) | 10039 | (1R)-1-Phenylethylamine; (1R)-1-Phenyl-1-ethanamine.; L-alpha-Phenylethylamine | 3886-69-9 | C8H11N | 详情 | 详情 |
Extended Information