Chloroform → 4-Oxo-4-(2-(5-(benzoxazol-2-yl)-2-methylbenzimidazol-1-yl)ethyl)aminobutyric acid

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Reaction Steps

1-(2-Aminoethyl)-5-(benzoxazol-2-yl)-2-methylbenzimidazole hydrochloride (see Working Example 56) (0.20 g, 0.6 mmol), succinic anhydride (0.06 g, 0.6 mmol), triethylamine (0.22 g, 2.2 mmol) and CHCl3 (2 mL) were added together, and after stirring for 1 hour at room temperature this was heated to reflux with stirring for 1 hour. After cooling, water was added and back-extraction was carried out. The aqueous layer obtained was concentrated, and the residue was reslurried in methanol. After the precipitated crystals were filtered, they were dried to yield the title compound (0.13 g, 69% yield) as white crystals.

Provenance & Evidence