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HRID 280574作成日:2026年10月24日
Amlodipine → 4-(2-Chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-{2-[(2-chloro-5-pyridyl)sulphonamido]ethoxymethyl}-1,4-dihydropyridine
https://huagongshe.com/ja/reaction/280574
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Amlodipine | HCID 2162 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 2-Chloro-5-pyridinesulfonyl chloride | HCID 2792792 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 4-(2-Chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-{2-[(2-chloro-5-pyridyl)sulphonamido]ethoxymethyl}-1,4-dihydropyridine | HCID 23320840 | 54.8% |
反応手順
A solution of 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine (409 mg) and triethylamine (202 mg) in dry dichloromethane (20 ml) was stirred under nitrogen and cooled in an ice-bath while a solution of 2-chloro-5-pyridinesulphonyl chloride (212 mg) in dry dichloromethane (10 ml) was added dropwise. The reaction mixture was allowed to warm to room temperature and stirring continued for a further 3 hours. The solvent was evaporated and the residue chromatographed on silica, eluting with dichloromethane. Appropriate fractions were combined and evaporated and the residue recrystallised from ethyl acetate to give the title compound (320 mg), m.p. 140°-140.5° C. Found: C, 51,27; H, 4.63; N, 7.25. C25H27Cl2N3O7 requires C, 51.37; H, 4.66; N, 7.19%.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US04590195 |
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| 出典データセット | uspto-grants-1986_05 |
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| ORD ID | ord-5c341f7cd88d44d39d32fefb43089a7a |
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| 出典メモ | uspto-grants-1986_05 |
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