反应详情

A mixture of 2-[5-(1-benzyloxycarbonyl-1,2,5,6-tetrahydropyridin-4-yl)-1-methyl-1H-indol-3-yl]-1-(toluene-4-sulfonyl)-1H-pyrrolo[2,3-b]pyridine (1.7 g, Reference Example 61) ethanol (53 mL) and palladium on carbon (0.35 g) was stirred in the presence of hydrogen for 4 hours, then left standing at room temperature overnight. After a further day a further quantity of palladium on carbon (0.18 g, 10%) was added and stirring was continued in the presence of hydrogen for a further 8 hours. After standing at room temperature for 4 days the reaction mixture was filtered through Hyflo and the filter pad was washed well with ethanol. The combined filtrate and washings was treated with palladium on carbon (0.35 g) and the mixture was stirred in the presence of hydrogen. The mixture was filtered through Hyflo and the filter pad was washed well with ethanol. The combined filtrate and washings was evaporated and the residue was subjected to flash chromatography on silica eluting with a mixture of ethyl acetate and pentane (4:1, v/v) to give the title compound as a light brown solid, m.p. 82-85° C.

1. waitleft
2. waitAfter standing at room temperature for 4 days
3. filtrationthe reaction mixture was filtered through Hyflo
4. washthe filter pad was washed well with ethanol
5. additionThe combined filtrate and washings was treated with palladium on carbon (0.35 g)
6. stirringthe mixture was stirred in the presence of hydrogen
7. filtrationThe mixture was filtered through Hyflo
8. washthe filter pad was washed well with ethanol
9. customThe combined filtrate and washings was evaporated
10. additionthe residue was subjected to flash chromatography on silica eluting with a mixture of ethyl acetate and pentane (4:1