Cesium carbonate → 1-[6-[(1,1-Dimethylethyl)amino]-2-pyrazinyl]-1H-benzimidazol-6-amine

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Reaction Steps

A mixture of 1H-benzimidazol-5-amine (2.93 g, 22 mmol), N-(tert-butyl)-6-chloropyrazin-2-amine (3.71 g, 20=not) and cesium carbonate (9.12 g, 28 mmol) in DMF (20 mL) was heated under N2 for 48 h. Upon cooling to RT the mixture was filtered and the filtrate concentrated in vacuo. The residue was extracted with CHCl3 and the solvent removed under reduced pressure. The residue was chromatographed using CH2Cl2-MeOH (98:2-93:7) to give from the less polar fractions 1-[6-(tert-butylamino)pyrazin-2-yl]-1H-benzimidazol-6-amine (1.38 g):

Provenance & Evidence