反应详情

4-p-tolyloxy-1H-indole-2-carboxylic acid (137) (850 mg, 3.2 mmol) and 4-amino-N-benzylpiperidine (605 mg, 3.2 mmol) are dissolved in 5 ml of DMF and after addition of TBTU (1.2 g, 3.5 mmol) and ethyldiisopropylamine (2.2 ml, 12.8 mmol) the mixture is stirred at room temperature for 2 h. Then the mixture is evaporated at high vacuum. The residue is dissolved in ethyl acetate and washed with saturated NaHCO3-solution and brine. The organic layers are dried over Na2SO4, filtrated and evaporated under reduced pressure. Yield: 1.47 g (100%) of a yellow foam. MS (ESI): 438 [M−H]−.

1. customThen the mixture is evaporated at high vacuum
2. dissolutionThe residue is dissolved in ethyl acetate
3. washwashed with saturated NaHCO3-solution and brine
4. dry with materialThe organic layers are dried over Na2SO4
5. filtrationfiltrated
6. customevaporated under reduced pressure