2-methyl-8-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuro[2,3-b]pyridine synthesis
- Product Name:2-methyl-8-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuro[2,3-b]pyridine
- CAS Number:1609374-04-0
- Molecular formula:C18H20BNO3
- Molecular Weight:309.17
![2-Methylbenzofuro[2,3-b]pyridin-8-yl trifluoromethanesulfonate](/CAS/20180527/GIF/1609373-98-9.gif)
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Yield:1609374-04-0 65%
Reaction Conditions:
with 1,1'-bis-(diphenylphosphino)ferrocene;(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride;potassium acetate in 1,4-dioxane at 80;
Steps:
3 3. Synthesis of intermediate I-1
2-methylbenzofuran [2,3-b]pyridin-8-yl-trifluoromethanesulfonate (20.0 g, 60.4 mmol), bis(pinacol) diboron (16.9 g, 66.4 mmol) KOAc (17.8 g, 181.1 mmol) was dissolved in 1,4-dioxane (300 mL), and Pd(dppf)Cl2 (3 mol%), dppf (3 mol%) was added.After heating to 80 ° C and stirring overnight, the reaction mixture was cooled to room temperature.It was diluted with water and extracted with ethyl acetate. The organic layer was separated, washed with brine, dried MgSO 4Concentrated column purification (9:1 = hexane: ethyl acetate)Intermediate I-1 (12.1 g, yield: 65%) was obtained.
References:
CN109810146,2019,A Location in patent:Paragraph 0083-0085
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