4-(3-Dimethylaminoazetidin-1-yl)piperidine-1-carboxylic acid [4-(2-fluoro-4-nitrophenoxy)pyridin-2-yl]amide → 4-(3-Dimethylaminoazetidin-1-yl)piperidine-1-carboxylic acid [4-(4-amino-2-fluorophenoxy)pyridin-2-yl]amide

Participants

Reaction Steps

To a solution of 4-(3-dimethylaminoazetidin-1-yl)piperidine-1-carboxylic acid [4-(2-fluoro-4-nitrophenoxy)pyridin-2-yl]amide (258 mg) in tetrahydrofuran (50 ml) was added 20% palladium hydroxide carbon (198 mg), followed by stirring under a hydrogen atmosphere at room temperature for 12 hrs. The reaction mixture was filtered to remove the catalyst, and the catalyst was washed with tetrahydrofuran:methanol=1:1. The filtrate was concentrated to provide the titled compound (236 mg, 97.8%) as a yellow amorphous substance.

Provenance & Evidence