Реакция #89339

Уравнение реакции

2-(((2S,3R)-1-(2-iodo-5-methylbenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

2-(tributylstannyl)pyrimidine

CsF

→

title compound

Выход 61.0%

2-(((2S,3R)-3-Methyl-1-(5-methyl-2-(pyrimidin-2-yl)benzoyl)piperidin-2-yl)methyl)isoindoline-1,3-dione

Выход 61.0%

Растворители

DMF

Условия реакции

Обработка

1. 1
   Другоеwas degassed
2. 2
   ДругоеThe solvent was removed in vacuo
3. 3
   Другоеto obtain the crude which
4. 4
   Другоеwas purified by silica gel chromatography (0˜100% EtOAc/hexanes)

Методика

A mixture of 2-(((2S,3R)-1-(2-iodo-5-methylbenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione (0.20 g, 0.40 mmol), 2-(tributylstannyl)pyrimidine (0.15 mL, 0.48 mmol), CsF (121 mg, 0.80 mmol), CuI (15 mg, 0.08 mmol) and Pd(PPh3)4 (46 mg, 0.04 mmol) in DMF (10 mL) was degassed and heated at 120° C. for 1 h in a microwave reactor. The solvent was removed in vacuo to obtain the crude which was purified by silica gel chromatography (0˜100% EtOAc/hexanes) to yield the title compound as a brown oil (0.11 g, 61%). MS (ESI) 455 (M+H).

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