反应详情

The title compound was prepared from 300 mg (0.672 mmol) 5-(1,3-dioxolan-2-yl)-3-iodo-1-{[2-(trimethylsilyl)ethoxy]methyl}-1H-indazole (Example 6A) in analogy to the procedure described in Example 21A. The procedure was modified by using 5 equivalents of 2-(morpholin-4-yl)ethanol as the alcohol reactant and by switching to toluene as solvent. After treating the mixture in a microwave oven at 140° C. for 2 h, the same amounts of catalyst and ligand were added again, and the mixture was refluxed for further 7 days using conventional heating. The crude product was purified by preparative RP-HPLC (acetonitrile/water gradient) to afford 93 mg (30% of th.) of the title compound.

1. additionAfter treating the mixture in a microwave oven at 140° C. for 2 h
2. additionthe same amounts of catalyst and ligand were added again
3. temperaturethe mixture was refluxed for further 7 days
4. customThe crude product was purified by preparative RP-HPLC (acetonitrile/water gradient)