反应详情

Charge a 50 mL flask equipped with a magnetic stir bar, 4-(7-chloro-imidazo[1,2-a]pyridin-3-yl)-benzylamine (720 mg, 2.79 mmol), di-isopropyl ethyl amine (723 mg, 0.93 mL, 5.6 mmol), and THF (28 mL). Purge the flask with N2, and add 3-trifluoromethylphenyl-isocyanate (1.04 g, 0.77 mL, 5.6 mmol) via syringe. Mix the reaction at room temperature for 24 hours. Evaporate the reaction in vacuo, and chromatograph the residue using SiO2 eluting with a gradient of 1% to 15% of 2 M NH3 in MeOH with the balance CH2Cl2. Evaporate the fractions containing the product under reduced pressure, and vacuum oven dry the resulting ivory solid at 40° C. to give the title compound 624 mg (50.3%). MS(ES), m/z 445.3 (M+1).

1. additionCharge a 50 mL flask
2. customequipped with a magnetic stir bar
3. customPurge the flask with N2
4. additionMix
5. customthe reaction at room temperature for 24 hours
6. customEvaporate
7. customthe reaction in vacuo, and chromatograph the residue
8. customEvaporate the fractions
9. additioncontaining the product under reduced pressure, and vacuum oven
10. customdry the resulting ivory solid at 40° C.