反应详情

To a stirred solution of (1-pyrrolo[2,3-b]pyridin-1-yl-cyclopentyl)-acetonitrile (399) (1.4 g, 6.21 mmol) in ethanol (50 mL) was added 50% aq. NH2OH (4 mL, 62.15 mmol) and the reaction mixture was heated at 60° C. for 16 h (TLC, 30% ethyl acetate in hexane, Rf=0.1). Ethanol was evaporated, water (50 mL) was added and the mixture was extracted with etylacetate (3×50 mL). The organic phase was thereafter dried and concentrated to get crude N-hydroxy-2-(1-pyrrolo[2,3-b]pyridin-1-yl-cyclopentyl)-acetamidine (400) (1.8 g, 112%) as an off-white sticky liquid.

1. customEthanol was evaporated
2. additionwater (50 mL) was added
3. extractionthe mixture was extracted with etylacetate (3×50 mL)
4. customThe organic phase was thereafter dried
5. concentrationconcentrated