反应详情

2-[2,4-Difluoro-3-[[2-fluoro-5-(3-fluorophenyl)phenyl]methylamino]phenoxy]acetic acid (I(b)) (70 mg, 0.17 mmol, 1.0 eq) was dissolved in iPrOH (5 mL). Concentrated sulphuric acid (2 drops) was added and the solution was stirred at room temperature overnight. The reaction was quenched by addition of aqueous NaHCO3 and the aqueous layer was extracted with EtOAc. The combined organic extracts were dried (MgSO4), filtered and evaporated in vacuo to give the crude product. The compound was triturated in a mixture of petroleum ether and DCM and dried under vacuum to give the title compound (II(d)) as a gummy solid (52 mg, 68%).

1. customThe reaction was quenched by addition of aqueous NaHCO3
2. extractionthe aqueous layer was extracted with EtOAc
3. dry with materialThe combined organic extracts were dried (MgSO4)
4. filtrationfiltered
5. customevaporated in vacuo
6. customto give the crude product
7. customThe compound was triturated in a mixture of petroleum ether and DCM
8. customdried under vacuum