反应详情

温度

70 °C

A mixture of 1-(3-chloropropyl)-5-(thiophen-2-yl)pyrimidine-2,4(1H,3H)-dione (Prep24, 50 mg, 0.18 mmol), 5-fluoro-2,3-dihydrospiro[indene-1,3′-pyrrolidine]hydrochloride salt (Prep14, 52 mg, 0.27 mmol), potassium carbonate (112 mg, 0.81 mmol), sodium iodide (112 mg, 0.75 mmol) and NMP (1 ml) was stirred at 70° C. overnight. The mixture was diluted with water and extracted with ethyl acetate. The EA phase was evaporated and the crude purified by preparative TLC to give the free base of the title compound (60 mg). the compound was purified by preparative HPLC and treated with a 1N solution of HCl-ether to give the title compound (6 mg, y=7%).

1. extractionextracted with ethyl acetate
2. customThe EA phase was evaporated
3. customthe crude purified by preparative TLC