反应详情

A mixture of 4-[6-chloro-4-(4-methanesulfonyl-phenoxy)-pyrazolo[3,4-d]pyrimidin-1-yl]-piperidine-1-carboxylic acid tert-butyl ester (Example 172; 230 mg, 0.45 mmol), trimethylaluminum (2 M in toluene; 0.5 mL, 1 mmol), and tetrakis(triphenyl-phosphine)palladium(0) (58 mg, 0.05 mmol) in tetrahydrofuran (5 mL) was heated at reflux for 2 h. The solvent was evaporated and the residue was purified by column chromatography to give 4-[4-(4-methanesulfonyl-phenoxy)-6-methyl-pyrazolo[3,4-d]pyrimidin-1-yl]-piperidine-1-carboxylic acid tert-butyl ester (93 mg, 42%) as a white foam/solid.

1. temperaturewas heated
2. temperatureat reflux for 2 h
3. customThe solvent was evaporated
4. customthe residue was purified by column chromatography