反应详情

3-(1H-indol-5-yl)-5-(4-(piperazin-1-ylmethyl)phenyl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine (50 mg) was dissolved in THF (1 mL) and treated with triethylamine (13 uL), and 2,2,2-trifluoroethyl methanesulfonate (13 uL); the reaction was allowed to stir for approximately hours, diluted water and extracted with EtOAC and washed with 1 N sodium hydroxide, water and brine and evaporated. The product was suspended in MeOH and (2 mL) detosylated directly by the addition of 0.5 mL sodium hydroxide solution, heated to 50 C for one hour. The reaction was diluted with water, extracted with dichloromethane and purified by MPLC, on silica gel, eluting with methanol in dichloromethane to yield 6 mg of an analytical sample (490 M+H).

1. extractiondiluted water and extracted with EtOAC
2. washwashed with 1 N sodium hydroxide, water and brine
3. customevaporated
4. addition(2 mL) detosylated directly by the addition of 0.5 mL sodium hydroxide solution
5. temperatureheated to 50 C for one hour
6. additionThe reaction was diluted with water
7. extractionextracted with dichloromethane
8. custompurified by MPLC, on silica gel
9. washeluting with methanol in dichloromethane
10. customto yield 6 mg of an analytical sample (490 M+H)