Water → HCID 136138825, compound

Participants

Reaction Steps

471 mg of N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride and 258 mg of (+)-(2,3-dihydro-1H-indol-2-yl)methanol (reference example 8a) are added to a solution of 470 mg of sodium (5-fluoro-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate in 14 ml of DMF and 14 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: 95/05 dichloromethane/methanol, so as to give 280 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