6-(2,6-Dichlorophenyl)-8-methyl-2-methylsulfonyl-8H-pyrido[2,3-d]pyrimidin-7-one → HCID 16657115, compound

Participants

Reaction Steps

A mixture of 0.384 g of compound of formula (II), 6-(2,6-dichlorophenyl)-8-methyl-2-methylsulfonyl-8H-pyrido[2,3-d]pyrimidin-7-one, and 0.266 g of compound of formula (III), (R/S)-2-(N-Boc-aminomethyl)-1,3-benzodioxol-5-ylamine, is heated in 4 ml of acetic acid at 80° C. for 2 h. The reaction medium is subsequently concentrated by half under vacuum, then taken up in water and ethyl acetate and brought to pH 6 with a saturated NaHCO3 solution; the organic phase is separated by settling, washed with water and then a saturated NaCl solution, dried over sodium sulfate and evaporated. The crude product obtained is purified by flash chromatography on silica with a gradient of 0 to 1% of methanol in dichloromethane. 0.252 g of expected product is obtained in the form of a yellow powder.

Provenance & Evidence