反应详情

温度

155 °C

To a suspension of 6-bromo-2-chloro-7-methyl-8-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridine (Int. 29, 125 mg, 0.32 mmol) in IMS (5 mL) was added 3-methylsulfanyl-propylamine (215 μL, 1.92 mmol) and the reaction mixture was heated under microwave irradiation at 155° C. for 2 hrs. After this time more 3-methylsulfanyl-propylamine (490 μL) was added and heating continued for 3 hrs then a further portion of 3-methylsulfanyl-propylamine (490 μL) was added and heating continued for 7 hrs. The resultant residue was loaded onto an SCX-2 cartridge and eluted with MeOH and then further purified by flash chromatography, eluting with a gradient of 0-50% EtOAc in cyclohexane to give the title compound as a colourless glass (57 mg).

1. temperatureheating
2. temperatureheating
3. waitcontinued for 7 hrs
4. washeluted with MeOH
5. customfurther purified by flash chromatography
6. washeluting with a gradient of 0-50% EtOAc in cyclohexane