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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

反応式

関与物質

役割名称HCID仕込み量
反応物AmlodipineHCID 2162—
反応物TriethylamineHCID 8471—
反応物2-Chloro-5-pyridinesulfonyl chlorideHCID 2792792—
溶媒DichloromethaneHCID 6344—
生成物4-(2-Chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-2-{2-[(2-chloro-5-pyridyl)sulphonamido]ethoxymethyl}-1,4-dihydropyridineHCID 2332084054.8%

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

DOI10.6084/m9.figshare.5104873.v1
特許番号US04590195
出典データセットuspto-grants-1986_05
ORD IDord-5c341f7cd88d44d39d32fefb43089a7a
出典メモuspto-grants-1986_05