反应详情

温度

100 °C

To a solution of 53-(benzyloxy)-5-bromopyridine 1-oxide (from step 2) (1.0 eq.) in acetonitrile (0.2 M) was added trimethylsilyl cyanide (TMSCN) (4.0 eq.) and triethylamine (3.0 eq.). The reaction was heated at 100° C. overnight. After cooling to room temperature, the solvent was concentrated en vacuo, and the residue was purified by a COMBIFLASH® system (ISCO) using 0-40% ethyl acetate in hexane to give a mixture of two benzoxy regioisomers, one of which was the desired product. The mixture was carried onto the next step without further purification.

1. temperatureAfter cooling to room temperature
2. concentrationthe solvent was concentrated en vacuo
3. customthe residue was purified by a COMBIFLASH® system (ISCO)
4. customto give
5. additiona mixture of two benzoxy regioisomers, one of which