Реакция #66742

Уравнение реакции

K3PO4

8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4′-piperidin]-1′-yl]carbonyl}quinolin-4-yl trifluoromethanesulfonate

[4-(methoxycarbonyl)phenyl]boronic acid

→

Methyl 4-(8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4′-piperidin]-1′-yl]carbonyl}quinolin-4-yl)benzoate

Растворители

MeCN

Условия реакции

Обработка

1. 1
   ФильтрацияThe mixture was filtered
2. 2
   Промывкаwashing with CHCl3
3. 3
   Другоеthe solvent was evaporated under reduced pressure
4. 4
   ДругоеThe residue was purified by silicagel column chromatography (hexane/EtOAc)
5. 5
   Другоеto give

Методика

K3PO4 (109 mg, 0.515 mmol) was added to a stirred mixture of TBAB (8.30 mg, 0.0260 mmol), PdCl2(dppf) (18.9 mg, 0.0260 mmol), 8-cyclopropyl-2-{[6-(1-methyl-1H-pyrazol-4-yl)-4-oxospiro[chroman-2,4′-piperidin]-1′-yl]carbonyl}quinolin-4-yl trifluoromethanesulfonate (165 mg, 0.258 mmol) and [4-(methoxycarbonyl)phenyl]boronic acid (55.6 mg, 0.309 mmol) in MeCN (2 ml) and the mixture was stirred at 90° C. overnight. The mixture was filtered, washing with CHCl3 and the solvent was evaporated under reduced pressure. The residue was purified by silicagel column chromatography (hexane/EtOAc) to give intended compound as a yellow solid.

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