Benzophenone imine → HCID 58997309, compound

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Reaction Steps

The (3-bromo-5-fluorophenyl)-methyl-(1-methylpiperidin-4-yl)-amine intermediate is then aminated at the benzo 3-position, as for example, by reacting the intermediate with BINAP, Pd2dba3, benzhydrylideneamine, and sodium t-butoxide, in a suitable solvent, such as toluene or the like, under an inert atmosphere for about 1–3 hr., say about 2 hr., at about 50° C. to 100° C., say about 80° C. The resulting intermediate is treated with 1M HCL or the like in a suitable solvent, such as THF at 0° C. to ambient temperature, preferably ambient temperature for 1–2 hours, say about 1 hr. The resulting intermediate, 5-Fluoro-N-methyl-N-(1-methylpiperidin-4-yl)benzene-1,3-diamine may then be isolated and purified by common procedures such as, but not limited to, solvent removal, extraction and/or chromatography, etc.

Provenance & Evidence