Dicyclohexylcarbodiimide → HCID 178486401, compound

Participants

Reaction Steps

To a mixture of methylene chloride (10 ml) and dimethylformamide (5 ml) are added the compound obtained in Example 128 (1.66 g), 1,3-dicyclohexyl carbodiimide (960 mg) and 1-hydroxybenzotriazole (710 mg), and the mixture is stirred at room temperature for 30 minutes. To the reaction mixture is added a solution of 4-(2-aminoethyl)imidazole (850 mg) and triethylamine (1.28 ml) in dimethylfomamide (5 ml), and the mixture is stirred for three hours, and then further stirred at 50° C. for 7 hours. To the reaction mixture are added water and ethyl acetate. The ethyl acetate layer is separated, washed, dried, and concentrated under reduced pressure. The residue is purified by silica gel column chromatography (solvent; chloroform:hexane=30:1) to give 6,7-dimethoxy-3-[2-(4-imidazolyl)ethylaminocarbonyl]-2-methyl-4-(3,4,5-trimethoxyphenyl)-1(2H)-isoquinolinone (1.0 g) as listed in Table 12.

Provenance & Evidence