反应详情

温度

40 °C

In a 40 mL septum capped vial purged with N2, add 4-(7-chloro-imidazo[1,2-a]pyridin-3-yl)-benzylamine (125 mg, 0.48 mmol), magnetic stir bar, CH2Cl2 (6 mL), cool the vial in an ice bath and slowly add 1 mL (CH2Cl2 solution of m-trifluoromethyl-phenylacetyl chloride, 0.48 mmol). Add isopropyl ethyl amine (0.8 mL) with THF (2 mL). Remove the vial from the ice bath and heat to 40° C. for 6 hours. Add a trace of MeOH and evaporate the solvents under vacuum and take up the oil into a minimal amount of CH2Cl2 and chromatograph using SiO2 eluting with a gradient of 0.5% to 5% of 2 M NH3 in MeOH with the balance CH2Cl2. Isolate the product, dry in a vacuum oven at 40° C. for 24 hours to give 144 mg (67%) MS (ES), m/z 444 (M+1).

1. custompurged with N2
2. temperaturecool the vial in an ice bath
3. customRemove the vial from the ice bath
4. additionAdd a trace of MeOH
5. customevaporate the solvents under vacuum
6. customIsolate the product
7. customdry in a vacuum oven at 40° C. for 24 hours
8. customto give 144 mg (67%)