반응 #1606360

반응 방정식

(3-((tert-butyldimethylsilyl)oxy)-4-cyclohexyl-2-fluorophenyl)boronic acid

5-bromopyrazin-2-amine

K2CO3

CH2Cl2

→

title compound

수율 101.3%

5-(3-((tert-Butyldimethylsilyl)oxy)-4-cyclohexyl-2-fluorophenyl)pyrazin-2-amine

수율 101.3%

용매

toluene

반응 조건

후처리

1. 1
   기타deoxygenated deionized water (10 mL)
2. 2
   온도The reaction mixture was then cooled to rt
3. 3
   workup.ADDITIONdiluted with dichloromethane (25 mL)
4. 4
   세척washed with brine (2×25 mL)
5. 5
   건조The organic layer was dried over MgSO4
6. 6
   여과filtered
7. 7
   농축concentrated to dryness

실험 절차

A mixture of (3-((tert-butyldimethylsilyl)oxy)-4-cyclohexyl-2-fluorophenyl)boronic acid (0.821 g, 2.33 mmol), 5-bromopyrazin-2-amine (0.40 g, 2.3 mmol), K2CO3 (0.659 g, 4.77 mmol), Pd(dppf)Cl2.CH2Cl2 (0.086 g, 0.12 mmol), deoxygenated toluene (10 mL), and deoxygenated deionized water (10 mL) was heated for 16 hours at 80° Celsius. The reaction mixture was then cooled to rt, diluted with dichloromethane (25 mL), and washed with brine (2×25 mL). The organic layer was dried over MgSO4, filtered, and concentrated to dryness to yield the title compound (0.936 g, 100%) which was used without purification.

출처