Cyanogen Bromide → 1-Cyclohexyl-5-[(piperidin-1-yl)methyl]-1H-benzimidazol-2-amine

Participants

Reaction Steps

N1-cyclohexyl-4-(piperidin-1-ylmethyl)benzene-1,2-diamine from step3 in methanol (200 mL) was added to a mixture of 5 M cyanogen bromide in acetonitrile (3.2 mL) and water (100 mL) dropwise over 1 hr with stirring. After 4.5 hr total reaction time, the mixture was evaporated to dryness. The residue was purified by preparative HPLC chromatography to yield 2.23 g of the title compound as the bis-TFA salt.

Provenance & Evidence