反応 #1606352

反応方程式

(3-((tert-Butyldimethylsilyl)oxy)-2-fluoro-4-methylphenyl)boronic acid

2-amino-5-bromopyrazine

Na2CO3

→

title compound

5-(3-((tert-Butyldimethylsilyl)oxy)-2-fluoro-4-methylphenyl)pyrazin-2-amine

溶媒

1,4-dioxane

反応条件

後処理

1. 1
   その他the resultant mixture sparged with argon for 10 minutes
2. 2
   workup.ADDITIONDCM was then added the mixture
3. 3
   温度The reaction mixture was then cooled to rt
4. 4
   workup.ADDITIONdiluted with water (5 mL)
5. 5
   抽出extracted with EtOAc (4×5 mL)
6. 6
   乾燥The combined organic extracts were then dried over Na2SO4
7. 7
   ろ過filtered
8. 8
   濃縮concentrated to dryness

実験手順

(3-((tert-Butyldimethylsilyl)oxy)-2-fluoro-4-methylphenyl)boronic acid (292 mg, 1.03 mmol), 2-amino-5-bromopyrazine (179 mg, 1.03 mmol), 1,4-dioxane (6.1 mL), and Na2CO3(2.1 mL, 2 M) were added to a microwave vial and the resultant mixture sparged with argon for 10 minutes. Pd(dppf)Cl2.DCM was then added the mixture, the vial sealed, and then heated at 80° Celsius for 16 hours. The reaction mixture was then cooled to rt, diluted with water (5 mL), and extracted with EtOAc (4×5 mL). The combined organic extracts were then dried over Na2SO4, filtered, and concentrated to dryness to provide the title compound. This compound was used directly in the next synthetic step without purification.

出典