Water → HCID 136196460, compound

Participants

Reaction Steps

890 mg of N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride and 500 mg of (+)-(2,3-dihydro-1H-indol-2-yl)methanol (reference example 13d) are added to a solution of 876 mg of sodium (4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate in 26 ml of DMF and 26 ml of pyridine. The reaction medium is stirred at ambient temperature for 18 hours 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 708 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