Pyridine → HCID 68281700, compound

Participants

Reaction Steps

0.19 g of N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride and 120 μl of pyridine are added to a solution of 0.22 g of sodium [1-methyl-4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate (prepared in step 2c of example 4c) in 3 ml of N,N-dimethylformamide. The resulting suspension is stirred at ambient temperature for 15 minutes and then 0.11 g of (+)-4-fluoro-2-methyl-2,3-dihydro-1H-indole [reference example 8c, step 6c] is rapidly added. The reaction mixture is stirred at ambient temperature for 64 hours and is then treated with a mixture of 20 ml of water and 2 ml of ethyl acetate, and then stirred at ambient temperature for 2 hours. The precipitate formed is filtered off, and then rinsed successively with 3 ml of water and 3×6 ml of diethyl ether. The solid obtained is dried with suction, then dried under reduced pressure at 40° C. 82 mg of (−)-2-{2-[4-fluoro-2-methyl-2,3-dihydro-1H-indol-1-yl]-2-oxoethyl}-3-methyl-6-(morpholin-4-yl)pyrimidin-4(3H)-one are thus obtained in the form of a white solid, the characteristics of which are the following:

Provenance & Evidence