Реакция #89481

Уравнение реакции

2-(((2S,3R)-1-(4,5-difluoro-2-iodobenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

2-(tributylstannyl)pyrimidine

CsF

→

title compound

2-(((2S,3R)-1-(4,5-Difluoro-2-(pyrimidin-2-yl)benzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione

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-(4,5-difluoro-2-iodobenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione (0.738 g, 1.409 mmol), 2-(tributylstannyl)pyrimidine (0.52, 1.409 mmol), CsF (0.43 g, 2.818 mmol), CuI (0.027 g, 0.14 mmol) and Pd(PPh3)4 (0.16 g, 0.14 mmol) in DMF (15 mL) was degassed and heated at 100° C. for 16 h. 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 white solid. MS (ESI) 477 (M+H).

Источник