反应详情

A mixture of N-(4-(3-iodopyridin-2-yloxy)phenyl)pyridin-2-amine (0.300 g, 0.771 mmol), copper(I) iodide (3.91 μL, 0.116 mmol), trans-dichlorobis(triphenyl-phosphine)palladium (II) (0.034 g, 0.048 mmol), triethylamine (0.800 mL, 5.74 mmol) and propargyl alcohol (0.150 mL, 2.54 mmol) in THF (5 mL) was stirred at rt under an atmosphere of argon for 3.5 h. The reaction was evaporated onto silica gel and purified by flash chromatography (Isco, (60 gram)) eluting with 2M NH3 in MeOH:CH2Cl2 (0:1→3:97). The material was stirred over MeOH, filtered and dried in vacuo to give a white crystalline solid. MS (ESI, pos. ion) m/z: 318.0. IC50 (uM)=0.2612.

1. customThe reaction was evaporated onto silica gel
2. custompurified by flash chromatography (Isco, (60 gram))
3. washeluting with 2M NH3 in MeOH:CH2Cl2 (0:1→3:97)
4. stirringThe material was stirred over MeOH
5. filtrationfiltered
6. customdried in vacuo
7. customto give a white crystalline solid