1-Benzylpiperazine → 7-(4-benzylpiperazin-1-yl)-N,N-dimethylbenzofuran-2-carboxamide

関与物質

反応条件

反応手順

The mixture of Tris(dibenzylideneacetone)dipalladium(0) (0.222 g, 0.24 mmol) and 2-Dicyclohexylphosphino-2',4',6'-tri-iso-propyl-1,1'-biphenyl (0.231 g, 0.48 mmol) in dioxane (10 mL) (degassed with argon for 5 min) was heated at 95 °C under argon for 5 min . This was transferred to a flask containing 7-bromo-N,N-dimethylbenzofuran-2-carboxamide (1.3 g, 4.85 mmol), 1-benzylpiperazine (1.111 g, 6.30 mmol) and Cesium carbonate (2.212 g, 6.79 mmol) in dioxane (10 mL) (degassed with argon for 5 min). The resulting mixture was heated at 95 °C over night. After cooling, the reaction mixture was filtered, the solid washed with DCM and concentrated. The product was purified by isco (DCM:MeOH; 0-3%). A small portion was also purified by prepLC giving EN02745-79-002.

情報源と証拠