(3-Nitro-pyridin-2-yl)-{4-[4-(3-pyrrolidin-1-yl-propoxy)-phenyl]-tetrahydro-pyran-4-ylmethyl}-amine → N*2*-{4-[4-(3-Pyrrolidin-1-yl-propoxy)-phenyl]-tetrahydro-pyran-4-ylmethyl}-pyridine-2,3-diamine

Participants

Reaction Steps

A solution of (3-Nitro-pyridin-2-yl)-{4-[4-(3-pyrrolidin-1-yl-propoxy)-phenyl]-tetrahydro-pyran-4-ylmethyl}-amine (465 mg, 1.06 mmol) in ethanol (˜10 mL) was hydrogenated for 4 hours at room temperature at 40 psi in the presence of 10% Pd/C (45 mg, 10% w/w). The reaction mixture was filtered over Arbocel® and rinsed with ethanol (30 mL), 2M HCl (20 mL) and EtOH (30 mL). The filtrate was concentrated in vacuo to give the title compound (365 mg, 84%). HRMS ESI+ m/z 411.2750 [MH]+.

Provenance & Evidence