反应详情

A suspension of 1-benzylspiro[indole-3,4′-piperidin]-2(1H)-one (0.417 mmol), 4-nitrophenyl chloroformate (84 mg, 0.417 mmol) and K2CO3 (172 mg, 1.25 mmol) in CH3CN (6 ml) is stirred at ambient temperature for 2 h. A solution of 1-cyclobutylpiperazine (0.417 mmol) and TEA (0.175 ml, 1.25 mmol) in CH3CN (4 ml) is added and the mixture is heated at 110° C. in a sealed tube overnight. Solvent is removed in vacuo and to the residue is added EtOAc (15 ml). The mixture is stirred at rt for 15 min and filtered. The filtrated is evaporated and the residue is purified by PTLC to give the title compound as a white solid. LC-MS (M+1): 458.3.

1. temperaturethe mixture is heated at 110° C. in a sealed tube overnight
2. customSolvent is removed in vacuo and to the residue
3. additionis added EtOAc (15 ml)
4. stirringThe mixture is stirred at rt for 15 min
5. filtrationfiltered
6. customThe filtrated is evaporated
7. customthe residue is purified by PTLC