반응 #85797

반응 방정식

4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid

Et3N

HOBt

morpholine

EDCl

→

title compound

수율 81.0%

Morpholino(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanone

수율 81.0%

용매

CH2Cl2

EtOAc H2O

반응 조건

후처리

1. 1
   추출extracted with EtOAc
2. 2
   세척The combined extracts were washed with brine
3. 3
   건조dried over anhydrous Na2SO4
4. 4
   여과filtered
5. 5
   농축concentrated
6. 6
   기타The residue was purified by flash chromatography

실험 절차

To a solution of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid (200 mg, 0.806 mmol) in CH2Cl2 (10 mL) was subsequently added EDCl (232 mg, 1.21 mmol), HOBt (163 mg, 1.21 mmol), morpholine (0.11 mL, 1.21 mmol), and Et3N (0.22 mL, 1.61 mmol). The mixture was stirred at room temperature overnight, treated with EtOAc/H2O, and extracted with EtOAc. The combined extracts were washed with brine, dried over anhydrous Na2SO4, filtered, and concentrated. The residue was purified by flash chromatography to give the title compound (207 mg, 81% yield). MS (m/z): 318 (M+H)+

출처