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HRID 622175作成日:2026年10月26日

Chloroform → Nicardipine Hydrochloride

https://huagongshe.com/reaction/622175

反応式

関与物質

役割名称HCID仕込み量
反応物ChloroformHCID 6212—
反応物DicyclohexylcarbodiimideHCID 10868—
反応物N-Benzyl-N-methylethanolamineHCID 66876—
反応物2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl esterHCID 173322—
生成物Nicardipine HydrochlorideHCID 4111485.4%

反応手順

A mixture of 3-methoxycarbonyl-2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-5-carboxylic acid (3.32 g, 0.01 mole), N-(2-hydroxyethyl)-N-benzyl-methylamine (4.98 g) and N,N'-dicyclohexylcarbodiimide (DCC) (2.05 g) is stirred at 60°-80° C. for 1 hour. To the reaction mixture chloroform (16 ml) is added and the mixture is washed with water (3×50 ml). Then the organic layer is washed with a 10% aqueous solution of HCl (16 ml) and water (3×10 ml). The organic layer is dried with anhydrous Na2SO4 and the solvent is evaporated in vacuo. The oily residue is dissolved in ethyl acetate (18 ml) and stirred at 0° C. for 2 hours. The precipitate, which separates, is filtered off, dried in vacuo and recrystallized from acetone. Thus, there is obtained the title compound nicardipine hydrochloride (4.4 g, 85.4%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US04769465
出典データセットuspto-grants-1988_09
ORD IDord-7b6da278485948ff8040dbb04421b14c
出典メモuspto-grants-1988_09