5-((2R,4S)-4-fluoro-2-(5-fluoro-2-(((S)-tetrahydrofuran-3-yl)oxy)phenyl)pyrrolidin-1-yl)-2-nitropyridine → 5-((2R,4S)-4-fluoro-2-(5-fluoro-2-(((S)-tetrahydrofuran-3-yl)oxy)phenyl)pyrrolidin-1-yl)pyridin-2-amine

Participants

Reaction Steps

To a stirred solution of 5-((2R,4S)-4-fluoro-2-(5-fluoro-2-(((S)-tetrahydrofuran-3-yl)oxy)phenyl)pyrrolidin-1-yl)-2-nitropyridine (5.1 g, 3.26 mmol) in ethanol (50 ml) was cooled to 10° C. and added Raney Ni (1.02 g, 20% w/w) portion wise and stirred for 5 min, then added N2H4.2H2O (3 ml) drop wise for the period of 5 min, then stirred for 20 min at room temperature. After completion of reaction, reaction mixture was filter through celite bed under N2 atmosphere and filtrate was concentration under reduced pressure, the residue was re-dissolved in DCM and washed with water, brine and dried over Na2SO4 and concentration to get desired product as brown solid (4.2 g, yield: 89%), MS (ESI): 362.1 (M+H).

Provenance & Evidence