반응 #1606352

반응 방정식

(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

용매

1,4-dioxane

반응 조건

후처리

1. 1
   기타the resultant mixture sparged with argon for 10 minutes
2. 2
   workup.ADDITIONDCM was then added the mixture
3. 3
   온도The reaction mixture was then cooled to rt
4. 4
   workup.ADDITIONdiluted with water (5 mL)
5. 5
   추출extracted with EtOAc (4×5 mL)
6. 6
   건조The combined organic extracts were then dried over Na2SO4
7. 7
   여과filtered
8. 8
   농축concentrated to dryness

실험 절차

(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.

출처