反应详情

温度

80 °C

Sitagliptin (4 g) and isopropanol (60 mL) are charged into a round-bottom flask and the mixture is heated to about 80° C. for about 30 minutes to obtain a clear dissolution. Fumaric acid (1.14 g) is added and the reaction mixture is refluxed for about 2 hours. The reaction mixture is cooled to about 30° C. and stirred for about 21 hours. The separated solid is filtered, washed with isopropanol (4 mL), and dried under reduced pressure at about 45° C. for about 2 hours to afford the title compound. (Yield: 4.0 g; MC: 1.05% w/w; HPLC purity: 99.47%)

1. customto obtain
2. dissolutiona clear dissolution
3. temperaturethe reaction mixture is refluxed for about 2 hours
4. temperatureThe reaction mixture is cooled to about 30° C.
5. filtrationThe separated solid is filtered
6. washwashed with isopropanol (4 mL)
7. customdried under reduced pressure at about 45° C. for about 2 hours