Water → HCID 136138825, compound

Participants

Reaction Steps

198 mg of N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride and 105 mg of (−)-(2,3-dihydro-1H-indol-2-yl)methanol (reference example 8a) are added to a solution of 207 mg of sodium (5-fluoro-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate in 6 ml of DMF and 6 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: 95/05 dichloromethane/methanol, so as to give 77 mg of 5-fluoro-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