反应详情

温度

60 °C

To a solution of methyl 5-fluoro-2-(3-((4-fluoro-2-methylphenyl)amino)azetidin-1-yl)nicotinate (D90) (150 mg, 0.450 mmol) in 1,4-dioxane/water (3 ml/1 ml), 1M NaOH (0.675 ml, 0.657 mmol) was added and the resulting mixture was stirred 2 h at 60° C. Organic solvent was evaporated. The remaining aqueous were washed with dichloromethane (5 ml) then acidified to pH2 by addition of 2M HCl and extracted with ethylacetate (3×20 ml). Collected organics, after solvent evaporation afforded the title compound (D135) (140 mg).

1. customOrganic solvent was evaporated
2. washThe remaining aqueous were washed with dichloromethane (5 ml)
3. additionthen acidified to pH2 by addition of 2M HCl
4. extractionextracted with ethylacetate (3×20 ml)
5. customCollected organics, after solvent evaporation