反応 #303144

反応方程式

Potassium phosphate

8-(5-bromo-2-fluorophenyl)-2-(cis-4-hydroxycyclohexyl)-2,8-diazaspiro[4.5]decan-1-one

2-(pyrrolidin-1-ylcarbonyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine

→

desired product

8-{2-Fluoro-5-[6-(pyrrolidin-1-ylcarbonyl)pyridin-3-yl]phenyl}-2-(cis-4-hydroxycyclohexyl)-2,8-di azaspiro[4.5]decan-1-one

溶媒

water

1,4-dioxane

反応条件

後処理

1. 1
   温度The resulting mixture was heated
2. 2
   ろ過The mixture was filtered
3. 3
   workup.ADDITIONThe filtrate was diluted with methanol
4. 4
   その他was purified by mass-guided reverse phase chromatography

実験手順

Potassium phosphate (0.017 g, 0.078 mmol) in water (0.10 mL) was added to a mixture of 8-(5-bromo-2-fluorophenyl)-2-(cis-4-hydroxycyclohexyl)-2,8-diazaspiro[4.5]decan-1-one (15.0 mg, 0.0353 mmol), 2-(pyrrolidin-1-ylcarbonyl)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine (16 mg, 0.053 mmol), and tetrakis(triphenylphosphine)palladium(0) (1.0 mg, 0.001 mmol) in 1,4-dioxane (0.30 mL). The resulting mixture was heated and stirred at 120° C. for 20 min. The mixture was filtered. The filtrate was diluted with methanol, and was purified by mass-guided reverse phase chromatography to afford the desired product. LCMS: (M+H)+=521.2.

出典