反应详情

2-Methyl-N-[1-(phenylsulfonyl)-6-(trimethylstannanyl)-1H-indazol-4-yl]-1,3-thiazole-4-carboxamide (1 g) was dissolved in DMF (4 ml) and 400 μl of the resultant solution was dispensed to 5-fluoro-4-iodo-1-[(4-nitrophenyl)sulfonyl]-1H-pyrrolo[2,3-b]pyridine (0.18 mmol) in DMF (400 μl) in a microwave vessel. Solvias catalyst (4 mg) was added and the reaction was heated in the microwave using initial 700 W to 135° C. for 20 min. The solution was loaded onto C18 SPE (pre-conditioned with 0.1% TFA in MeCN) and flushed through with 0.1% TFA in MeCN (3 ml). The solvent was removed under nitrogen blowdown. The sample was dissolved in DMSO (0.5 ml) and purified by MDAP (method D). The solvent was evaporated in vacuo using the Genevac. The sample was dissolved in IPA (300 μl) and 2M NaOH (aq) (300 μl) was added. The reaction was left overnight. The sample was dissolved in DMSO (0.6 ml) and purified by MDAP (method M). The solvent was evaporated in vacuo using the Genevac to give title compound, 2 mg.

1. temperaturethe reaction was heated in the microwave
2. customfor 20 min
3. customflushed through with 0.1% TFA in MeCN (3 ml)
4. customThe solvent was removed under nitrogen
5. dissolutionThe sample was dissolved in DMSO (0.5 ml)
6. custompurified by MDAP (method D)
7. customThe solvent was evaporated in vacuo
8. dissolutionThe sample was dissolved in IPA (300 μl)
9. addition2M NaOH (aq) (300 μl) was added
10. dissolutionThe sample was dissolved in DMSO (0.6 ml)
11. custompurified by MDAP (method M)
12. customThe solvent was evaporated in vacuo