Water → HCID 136196460, compound

Participants

Reaction Steps

673 mg of N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride and 378 mg of (−)-(2,3-dihydro-1H-indol-2-yl)methanol (reference example 13d) are added to a solution of 640 mg of sodium (4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate in 20 ml of DMF and 20 ml of pyridine. The reaction medium is stirred at ambient temperature for 18 hours and then a mixture of water and dichloromethane is added. After settling out, the organic phase is dried over magnesium sulfate, filtered, and then concentrated under reduced pressure. The residue obtained is purified on a silica column, eluent: gradient: dichloromethane/methanol from 100/0 to 95/05, so as to give 456 mg of 2-[2-((+)-2-hydroxymethyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one, the characteristics of which are the following:

Provenance & Evidence