2-Methoxyethylamine → 1-(2-aminopyrimidin-4-yl)-6-bromo-N-(2-methoxyethyl)-1H-1,3-benzodiazol-2-amine

Participants

Reaction Steps

A mixture of 4-[6-bromo-2-(trichloromethyl)-1H-1,3-benzodiazol-1-yl]pyrimidin-2-amine (1.5 g, 3.68 mmol) and cesium carbonate (2.5 g, 7.67 mmol) in 2-methoxyethan-1-amine (15 mL) was stirred under nitrogen for 3 days at room temperature. The reaction mixture was concentrated under vacuum and the residue was purified on a C18 column (acetonitrile/water, 5:95-80:20) to give 0.55 g (39%) of 1-(2-aminopyrimidin-4-yl)-6-bromo-N-(2-methoxyethyl)-1H-1,3-benzodiazol-2-amine as a yellow solid. LC-MS: m/z=+363 (M+H)+.

Provenance & Evidence