反应详情

3-[(E)-2-(4-Fluorophenyl)-vinyl]-4-methoxy-1H-indazole-5-carboxylic acid obtained by Example 234 and 258 mg of glycine ter-butyl ester hydrochloride were dissolved in 20 mL of N,N-dimethylformamide, and 0.871 mL of diisopropylethylamine and 235 mg of 1-hydroxybenzotriazole were added, and stirred at room temperature for 10 minutes. After cooling to 0° C., 491 mg of WSC hydrochloride was added, and stirred overnight at room temperature. After adding ice water to stop the reaction, the solution was extracted with ethyl acetate. The organic phase was washed with water and saturated brine and dried over anhydrous magnesium sulfate. The solvent was evaporated, to afford 547 mg of the title compound as pale green crystals.

1. temperatureAfter cooling to 0° C.
2. stirringstirred overnight at room temperature
3. customthe reaction
4. extractionthe solution was extracted with ethyl acetate
5. washThe organic phase was washed with water and saturated brine
6. dry with materialdried over anhydrous magnesium sulfate
7. customThe solvent was evaporated