Реакция #49469

Уравнение реакции

tri(o-tolyl)phosphine

triethylamine

7-iodo-4-methylisoindolinone

7-iodoisoindolinone

7-aminoisoindolinone

4-methyl-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

→

7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

Выход 56.0%

Растворители

acetonitrile

Условия реакции

Обработка

1. 1
   Другоеfollowed by purification by preparative thin-layer chromatography (chloroform/methanol=12/1)
2. 2
   Другоеto obtain

Методика

In a similar manner to Step 2 of Example 1, a mixture of 7-iodo-4-methylisoindolinone and 7-iodoisoindolinone (10/1, 40.5 mg, 0.149 mmol) was dissolved in acetonitrile (3.24 mL), and the solution was treated with Compound BD (107 mg, 0.298 mmol), palladium acetate (2.7 mg, 0.012 mmol), tri(o-tolyl)phosphine (7.3 mg, 0.024 mmol) and triethylamine (0.208 mL, 1.49 mmol), followed by purification by preparative thin-layer chromatography (chloroform/methanol=12/1) to obtain a mixture of 4-methyl-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone and 7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone (38.2 mg, ratio 92.9/7.1, yield 56%). 4-methyl-7-[1-(tert-butoxycarbonyl)-5-(piperidinomethyl)indol-2-yl]isoindolinone

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