Sodium Iodide → HCID 24751513, compound

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of 1-[4-(5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-2-yl)-phenyl]-ethanone (253 mg, 1.0 mmol) in acetonitrile (5.0 ml) is added 2-chloro-(4-cyclobutyl-piperazine)-acetamide (216 mg, 1.0 mmol, 1.0 eq.), K2CO3 (276 mg, 2.0 mmol, 2.0 eq.) and NaI (50 mg). The resulting mixture is stirred at 50° C. overnight. Water (10.0 ml) is added to quench the reaction, and the acetonitrile is evaporated. The residue is extracted with DCM (10 ml×3), and the combined organic phase is dried over sodium sulfate and concentrated. The residue is purified by preparative silica gel flash chromatography (EtOAc/4% TEA) to give the title compound. 1H NMR (300 MHz, CDCl3) δ 8.52 (2H, d), 8.48 (1H, s), 8.05 (2H, d), 3.78 (2H, s), 3.58˜3.72 (4H, m), 3.45 (2H, s), 3.09 (2H, t), 2.97 (2H, t), 2.69 (1H, m), 2.65 (3H, s), 2.29 (4H, m), 1.66˜2.08 (6H); MS (+VE) m/z 434.2 (M++1).

Provenance & Evidence