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HRID 280571作成日:2026年10月24日

Amlodipine → 4-(2-Chlorophenyl)-3-ethoxycarbonyl-2-[2-(imidazolidin-2-on-1-ylcarbonylamino)ethoxymethyl]-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine

https://huagongshe.com/ja/reaction/280571

反応式

関与物質

役割名称HCID仕込み量
反応物AmlodipineHCID 2162—
反応物2-Oxoimidazolidine-1-carbonyl chlorideHCID 83241—
溶媒ChloroformHCID 6212—
溶媒TriethylamineHCID 8471—
生成物4-(2-Chlorophenyl)-3-ethoxycarbonyl-2-[2-(imidazolidin-2-on-1-ylcarbonylamino)ethoxymethyl]-5-methoxycarbonyl-6-methyl-1,4-dihydropyridineHCID 2332083455.4%

反応手順

To a solution of 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine (1.0 g) in a mixture of chloroform (dried over alumina) (20 ml) and triethylamine (2 ml) was added imidazolidin-2-on-1-yl carbonyl chloride (0.36 g) in one portion and the mixture stirred at room temperature for 18 hours. After evaporation to dryness, the resultant oil was partitioned between 5% aqueous sodium carbonate and methylene chloride. The combined organic liquors were dried (MgSO4), filtered and evaporated to give 0.7 g of a yellow oil which crystallised from diisopropyl ether on standing to give pure title compound, (0.4 g), m.p. 145° C. Found: C, 54.94; H, 5.62; N, 10.62. C24H29ClN4O7 requires C, 55.33; H, 5.61; N, 10.76%.

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-8d6285e2a19844b09cd01ee36e7060af
出典メモuspto-grants-1986_05