A kind of indole derivative of pyridine piperidine indole ring structure and its synthesis method
A technology for indole derivatives and pyridine piperidine, which is applied to indole derivatives of pyridine piperidine indolo ring structure and the field of synthesis thereof, can solve the problems of low yield, complicated steps and the like, and achieves simple steps and high yield. The effect of high, high biological activity and medicinal value
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Embodiment 1
[0029] A kind of indole derivative of pyridine piperidine indole ring structure, its general chemical structure formula is:
[0030]
[0031] The synthetic method of the indole derivative of above-mentioned pyridine piperidine indole ring structure, comprises the following steps:
[0032] (1) Under nitrogen protection, 0.20 mmol of N-pyridyl indole, 0.2 mmol of toluene, and cobalt catalyst CoCp (CO)I were sequentially added into the schlenk tube. 2 1.8mol%, silver acetate AgOAc 3.6mol%, copper acetate monohydrate Cu(OAc) 2 ·H 2 O 0.22 mmol, silver tetrafluoroborate, AgBF 4 0.22mmol and 1,2-dichloroethane 3mL;
[0033] (2) Place the reaction tube in step (1) under the condition of an oil bath at 130° C. and stir for 30 hours;
[0034] (3) After the reaction is completed, the reaction tube is cooled to room temperature, the reaction mixture is desalted, washed with dichloromethane, concentrated, and purified by column chromatography. The column chromatography conditions...
Embodiment 2
[0038] A kind of indole derivative of pyridine piperidine indole ring structure, its general chemical structure formula is:
[0039]
[0040] The synthetic method of the indole derivative of above-mentioned pyridine piperidine indole ring structure, comprises the following steps:
[0041] (1) Under the protection of nitrogen, 0.20 mmol of N-pyridyl indole, 0.22 mmol of toluene, and cobalt catalyst CoCp (CO)I were sequentially added into the schlenk tube. 2 2.0mol%, silver acetate AgOAc 4.0mol%, copper acetate monohydrate Cu(OAc) 2 ·H 2 O 0.20 mmol, silver tetrafluoroborate, AgBF 4 0.20mmol and 1,2-dichloroethane 2mL;
[0042] (2) Place the reaction tube in step (1) under the condition of an oil bath at 135° C. and stir for 24 hours;
[0043] (3) After the reaction is completed, the reaction tube is cooled to room temperature, the reaction mixture is desalted, washed with dichloromethane, concentrated, and purified by column chromatography. The column chromatography co...
Embodiment 3
[0047] A kind of indole derivative of pyridine piperidine indole ring structure, its general chemical structure formula is:
[0048]
[0049] The synthetic method of the indole derivative of above-mentioned pyridine piperidine indole ring structure, comprises the following steps:
[0050] (1) Under the protection of nitrogen, 0.20 mmol of N-pyridyl indole, 0.22 mmol of toluene, and cobalt catalyst CoCp (CO)I were sequentially added into the schlenk tube. 2 2.0mol%, silver acetate AgOAc 4.0mol%, copper acetate monohydrate Cu(OAc) 2 ·H 2 O 0.20 mmol, silver tetrafluoroborate, AgBF 4 0.20mmol and 1,2-dichloroethane 2mL;
[0051] (2) Place the reaction tube in step (1) under the condition of an oil bath at 135° C. and stir for 24 hours;
[0052] (3) After the reaction is completed, the reaction tube is cooled to room temperature, the reaction mixture is desalted, washed with dichloromethane, concentrated, and purified by column chromatography. The column chromatography co...
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