Tetrahydrofuran → Benzimidazol-2-one

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Reaction Steps

In Scheme I, 2-fluoro-nitrobenzene is reacted with a primary amine, intermediate (h), wherein R1 is as described herein, to provide intermediate (i), which is reduced to a diaminophenyl, intermediate (j). The diaminophenyl is reacted with carbonyldiimidazole in the presence of an inert diluent, such as tetrahydrofuran, at a temperature range of from about 20° C. to about 40° C. for between about 12 and about 30 hours, to provide a benzoimidazolone compound of intermediate (d). A representative synthesis of a compound of intermediate (d) is described herein in Example 1, steps (a)-(c).

Provenance & Evidence