反应详情

温度

60 °C

(S)-tetrahydrofuran-3-yl 3-(2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-ylamino)azetidine-1-carboxylate, 6d, was dissolved in methanol (2 mL) and then treated with of 25% sodium methoxide/methanol (0.5 mL) and heated at 60° C. in sealed tube. LCMS showed complete reaction after 10 minutes. The resulting solution was quenched with aqueous saturated NH4Cl solution (0.5 mL) then evaporated to dryness and the residue dissolved in DMSO and purified by reverse phase HPLC (ammonium formate buffer) to afford 25.9 mg (55% yield) of the desired product, 422, as a solid.

1. customreaction after 10 minutes
2. customThe resulting solution was quenched with aqueous saturated NH4Cl solution (0.5 mL)
3. customthen evaporated to dryness
4. dissolutionthe residue dissolved in DMSO
5. custompurified by reverse phase HPLC (ammonium formate buffer)