3-Methoxypropyne → 4-(3-Methoxy-1-propinyl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

참여 물질

반응 단계

In a similar manner to Step 2 of Example 161, 4-trifluoromethanesulfonyloxy-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (400 mg, 0.674 mmol) was dissolved in diethylamine (16 mL), and the solution was treated with bis(triphenylphosphine)dichloropalladium (56.7 mg, 0.012 mmol), copper iodide (46.2 mg, 0.243 mmol) and methyl propargyl ether (0.398 mL, 4.72 mmol), followed by purification by preparative thin-layer chromatography (chloroform/methanol=6/1 to 8/1) to obtain 4-(3-methoxy-1-propinyl)-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (250 mg, yield 72%).

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