Hydrochloric Acid → 2-Aminopyridinoyl-piperidine

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Reaction Steps

Next, the 2-chloropyridinoyl-piperidine intermediate is reacted with benzophenone imine in the presence of tris(dibenzylidineacetone)-dipalladium(0) Pd2(dba)3) as a catalyst, and 2,2′-bis(diphenylphosphino)-1,1′binaphthyl (BINAP) and sodium t-butoxide in a suitable solvent, such as toluene, at reflux, to substitute the halo group with the benzophenone imino group. After work-up, this intermediate is typically reacted with hydrochloric acid in a suitable solvent, such as tetrahydrofuran, and then purified to give the corresponding 2-aminopyridinoyl-piperidine intermediate.

Provenance & Evidence