反应详情

To a solution of 3-(2-aminoethyl)-2-(3,5-dimethylphenyl)-1H-indole-5-carboxylic acid diisopropylamide in a mixture of dry chloroform and methanol at 0° C. is added magnesium sulfate followed by 2.5 equivalents of 5-pyridin-3-yl-thiophene-2-carbaldehyde and the mixture stirred at low temperature. After 40 minutes, acetic acid is added followed by a solution of sodium cyanoborohydride and the mixture allowed to warm to room temperature. After completion, the reaction is quenched by the addition of saturated aqueous sodium bicarbonate, extracted with methylene chloride and the combined organics washed sequentially with water and brine. Purification of the concentrate by preparative tlc on silica gel gives the title compound.

1. customAfter completion, the reaction is quenched by the addition of saturated aqueous sodium bicarbonate
2. extractionextracted with methylene chloride
3. washthe combined organics washed sequentially with water and brine
4. customPurification of the
5. concentrationconcentrate by preparative tlc on silica gel