反应详情

To a mixture of methyl [1-((2R)-2-{[(4-fluorophenyl)sulfonyl](methyl)amino}-4-oxobutyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]acetate (272 g, 589 mmol) in ethyl acetate (2.5 L) was added PPTS (326.33 g, 1299 mmol). After a period of 4 days at 65° C., the reaction mixture was quenched with saturated sodium bicarbonate and extracted with ethyl acetate. The organic phase was separated, washed with brine, dried over sodium sulfate, filtered and evaporated under reduced pressure. The residue was purified by combiflash (10% ethyl acetate in hexane to 100% ethyl acetate) to give the title compound.

1. customthe reaction mixture was quenched with saturated sodium bicarbonate
2. extractionextracted with ethyl acetate
3. customThe organic phase was separated
4. washwashed with brine
5. dry with materialdried over sodium sulfate
6. filtrationfiltered
7. customevaporated under reduced pressure
8. customThe residue was purified by combiflash (10% ethyl acetate in hexane to 100% ethyl acetate)