Water → HCID 18399126, compound

Participants

Reaction Steps

The compound obtained in Example 66 (1.0 g), dimethylaminopyridine (26 mg) and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (448 mg) are dissolved in a mixture of methylene chloride (20 ml) and methanol (340 ml). The mixture is stirred at room temperature for 10 minutes, and thereto are added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (41 mg) and dimethylaminopyridine (26 mg), and the mixture is stirred at room temperature overnight. To the reaction mixture are added water and ethyl acetate, and the ethyl acetate layer is washed, dried, and concentrated under reduced pressure. The residue is purified by silica gel column chromatography (solvent; hexane:ethyl acetate=2:1) to give 2-(tert-butoxycarbonylamino)-3-methoxycarbonyl-4-(3,4,5-trimethoxyphenyl)-1(2H)-isoquinolinone (438 mg) as listed in Table 6.

Provenance & Evidence