1-(5-Nitropyridin-2-yl)azetidin-3-ol → 1-(5-Aminopyridin-2-yl)azetidin-3-ol

Participants

Reaction Steps

A suspension of 0.34 g (1.74 mmol) of 2-(3-hydroxyazetidin-1-yl)-5-nitropyridine, prepared in the preceding stage, and of 9 mg of Pd/C at 10% in 10 ml of ethanol is stirred vigorously at 20° C. under 5 atmospheres of hydrogen for 4 hours. After this period of time, the mixture is filtered through a celite buffer and then concentrated under reduced pressure. The resulting product is purified by silica column chromatography, elution being carried out with a mixture of dichloromethane and methanol. 0.1 g of the expected product is thus obtained, which product will be used as it is in the subsequent synthesis.

Provenance & Evidence