4-(Morpholin-4-ylcarbonyl)-1-(propylsulfonyl)piperidine-4-carbonitrile → {[4-(Morpholin-4-ylcarbonyl)-1-(propylsulfonyl)piperidin-4-yl]methyl}amine

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Reaction Steps

A mixture of 4-(morpholin-4-ylcarbonyl)-1-(propylsulfonyl)piperidine-4-carbonitrile (I-4) (3.29 g, 10 mmole) and Raney Ni (2 g) in 2M NH3-MeOH (100 mL) was hydrogenated (55 psi) overnight at room temperature. Next morning, LCMS indicated that the hydrogenation was completion. Raney Ni was filtered and washed with MeOH (5×60 mL). The collected MeOH solution was concentrated to afford the title amine (I-5) (3.29 g, 99%) as a white solid. Analytical LCMS: single peak (214 nm), 1.723 min.

Provenance & Evidence