反应详情

To a solution of 2.21 g of methyl 6-piperazinylnicotinate (compound 6), 3.18 g of sodium carbonate and 1.64 g of cyclopentyl bromide in 50 ml of DMF was added a catalytic amount of NaI. The mixture was heated to 120°-130° C. and stirred for 4 hours. The resulting mixture was poured into 150 ml of water and extracted with ethyl acetate. The extract was washed twice with water, and once with a saturated aqueous sodium chloride solution, then dried over anhydrous magnesium sulfate and concentrated. Purification of the concentrate by column chromatography (silica gel; ethyl acetate) afforded 1.73 g of methyl 6-(4 -cyclopentyl-1-piperazinyl)nicotinate (yield 60%).

1. temperatureThe mixture was heated to 120°-130° C.
2. extractionextracted with ethyl acetate
3. washThe extract was washed twice with water
4. dry with materialonce with a saturated aqueous sodium chloride solution, then dried over anhydrous magnesium sulfate
5. concentrationconcentrated
6. customPurification of the
7. concentrationconcentrate by column chromatography (silica gel; ethyl acetate)