反应详情

To 122D (750 mg, 2.8 mmol) in THF (10 mL) was added n-BuLi (1.6M in hexane, 2.3 mL) at −78° C. After stirring for 10 min, trimethyl borate (0.63 mL) was introduced. The mixture was stirred from −78° C. to rt for 3 h before it was quenched by 1N HCl and extracted with ethyl acetate. The organic extracts were washed with saturated Na2S2O3, brine and dried over MgSO4. Evaporation of the solvent gave product 122E (356 mg, 69% yield) as a solid. 1H NMR (400 MHz, CDCl3) δ ppm 2.18 (s, 3H) 3.80 (s, 3H) 6.80-6.86 (m, 2H).

1. stirringThe mixture was stirred from −78° C. to rt for 3 h before it
2. customwas quenched by 1N HCl
3. extractionextracted with ethyl acetate
4. washThe organic extracts were washed with saturated Na2S2O3, brine
5. dry with materialdried over MgSO4
6. customEvaporation of the solvent