Iodine → 7-Iodo-4-(thiophen-2-yl)isoindolinone

Participants

Reaction Steps

In a similar manner to Step 4 of Example 140, 7-amino-4-(thiophen-2-yl)isoindolinone (212 mg, 0.920 mmol) was dissolved in acetonitrile (14.8 mL), and the solution was treated with potassium iodide (183 mg, 1.10 mmol), copper iodide (210 mg, 1.10 mmol), iodine (280 mg, 1.10 mmol) and tert-butyl nitrite (0.382 mL, 2.76 mmol), followed by purification by preparative thin-layer chromatography (chloroform/acetonitrile-6/1, chloroform/methanol=10/1) to obtain 7-iodo-4-(thiophen-2-yl)isoindolinone (138 mg, yield 44%).

Provenance & Evidence