反应详情

To a stirred degassed solution of 2-(1-{1H-pyrrolo[2,3-b]pyridin-1-yl}cyclopentyl)ethanimidamido acetate (401) (500 mg, 1.67 mmol) in ethanol (20 mL) was added 10% Pd—C (50 mg) and stirring was continued 30 min under H2 (hydrogen-bludder) at room temperature (TLC, 50% ethyl acetate in hexane, Rf=0.1), The reaction mixture was filtered through a celite bed and washed with 10% methanol in dichloromethane (5×50 mL). The organic phase was thereafter dried and concentrated to get 2-(1-pyrrolo[2,3-b]pyridin-1-yl-cyclopentyl)-acetamidine; compound with acetic acid (402) (437 mg, 87%) as an off-white solid.

1. filtration(TLC, 50% ethyl acetate in hexane, Rf=0.1), The reaction mixture was filtered through a celite bed
2. washwashed with 10% methanol in dichloromethane (5×50 mL)
3. customThe organic phase was thereafter dried
4. concentrationconcentrated