Hydrochloric Acid → 2-Oxo-3-[1-(tetrahydro-2H-pyran-4-yl)-4-piperidinyl]-2,3-dihydro-1H-benzimidazole-5-carbonitrile hydrochloride

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Reaction Steps

4-Amino-3-{[1-(tetrahydro-2H-pyran-4-yl)-4-piperidinyl]amino}benzonitrile (D59, 240 mg, 0.0008 mol, 1 eq), diisopropylethylamine (140 mg, 0.00104 mol, 1.3 eq), triphosgene (70 mg, 0.00024 mol, 0.3 eq), and dichloroethane (20 ml) were combined. After 5 min, 4 ml of 4M HCl in dioxane were added, the reaction evaporated, the residue dissolved in methanol and purified exactly as in Example 1, where A=H2O and B=CH3CN to produce the title compound as a white solid. MS (ESI): 327 [M+H]+.

Provenance & Evidence