6-(2,6-Dichlorophenyl)-8-methyl-2-methylsulfonyl-8H-pyrido[2,3-d]pyrimidin-7-one → 6-(2,6-dichlorophenyl)-2-[(2,3-dihydro-6-benzofuranyl)amino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one

Participants

Reaction Steps

1 g of compound of formula (II), 6-(2,6-dichlorophenyl)-8-methyl-2-methylsulfonyl-8H-pyrido[2,3-d]pyrimidin-7-one, and 352 mg of the compound of formula (III), (2,3-dihydro-6-benzofuranyl)amine, are heated at 80° C. in 10 ml of acetic acid for 1 h 30. After returning to ambient temperature, the medium is filtered in order to remove an impurity, diluted with water and ethyl acetate and brought to pH 9 with NaHCO3. The organic phase is then washed with a saturated NaCl solution, dried over Na2SO4 and concentrated under vacuum. The residue is chromatographed on silica (gradient: heptane 100 to heptane/ethyl acetate 40:60) to give 201 mg of the expected product in the form of a yellow solid.

Provenance & Evidence