反应详情

Sodium borohydride (2.2 g, 58.34 mmol) was added at 0° C. portion wise to a suspension of 6-(morpholine-4-carbonyl)-1H-indole-3-carbaldehyde (5 g, 19.44 mmol) in methanol (106 mL) and the mixture was stirred at room temperature for 3 h. The methanol was removed under vacuum whereby the temperature was kept below <35° C. The residue was diluted with water (100 mL) and extracted with ethyl acetate (3×100 mL). The combined organic layers were washed with brine, dried over sodium sulfate and evaporated. Washing of the remnant with ether provided the product as white solid. Yield: 4 g (79% of theory)

1. customThe methanol was removed under vacuum whereby the temperature
2. customwas kept below <35° C
3. additionThe residue was diluted with water (100 mL)
4. extractionextracted with ethyl acetate (3×100 mL)
5. washThe combined organic layers were washed with brine
6. dry with materialdried over sodium sulfate
7. customevaporated
8. washWashing of the remnant with ether