反应详情

Lithium 7-(4-(2-(pyridin-2-yl)ethyl)piperazin-1-yl)benzofuran-2-carboxylate (0.060 g, 0.17 mmol) was dissolved in dry DMF (1.7 mL), and then TSTU (0.064 g, 0.21 mmol) was added followed by triethylamine (0.059 mL, 0.43 mmol). The reaction was stirred for 15 min then 2-picolylamine (0.019 mL, 0.19 mmol) was added. The reaction was stirred at room temperature under argon over night. The crude product was purified by preparative LC. The fractions were combined and the acetonitrile was evaporated. DCM was added and the layers separated. The aq phase was extracted with DCM (3×). The combined organic phases were dried (Na2SO4), filtered and evaporated to give 37 mg (49%) of the title compound.

1. stirringThe reaction was stirred at room temperature under argon over night
2. customThe crude product was purified by preparative LC
3. customthe acetonitrile was evaporated
4. additionDCM was added
5. customthe layers separated
6. extractionThe aq phase was extracted with DCM (3×)
7. dry with materialThe combined organic phases were dried (Na2SO4)
8. filtrationfiltered
9. customevaporated