Trimethyl orthoacetate → 5-(Benzoxazol-2-yl)-2-methyl-1-cyclopropylbenzimidazole

Participants

Reaction Steps

To a methanol (5 mL) solution of 2-(2-cyclopropylaminoanilin-5-yl)benzoxazole (see Working Example 53-1) (140 mg, 0.425 mmol) was added 1,1,1-trimethoxyethane (75 mg, 0.624 mmol), and this was stirred at room temperature for 6 hours. After the reaction was complete, this was concentrated, and the residue obtained was purified by silica gel column chromatography to yield the imidazole (63.5 mg, 42% yield).

Provenance & Evidence