反应详情

To a solution of 5-(5-(3-chloropropylthio)-4-methyl-4H-1,2,4-triazol-3-yl)-2,4-dimethylthiazole (Prep28, 70 mg, 0.23 mmol) in dry NMP (1 ml), K2CO3 (0.145 g, 1.05 mmol) was added and stirred for 10 min. Then 5-fluoro-2,3-dihydrospiro[indene-1,3′-pyrrolidine]hydrochloride salt (Prep14, 88 mg, 0.39 mmol) and NaI (0.07 g, 0.47 mmol) were added and stirred overnight at 65° C. Water was then added and the solution was extracted with ethyl acetate (2×10 ml). The organic phase was washed with brine, dried over Na2SO4 and concentrated in vacuo. The crude product was purified by P-HPLC to give 38 mg of the title compound (y=36%).

1. stirringstirred overnight at 65° C
2. extractionthe solution was extracted with ethyl acetate (2×10 ml)
3. washThe organic phase was washed with brine
4. dry with materialdried over Na2SO4
5. concentrationconcentrated in vacuo
6. customThe crude product was purified by P-HPLC