Benzophenone imine → HCID 66939208, compound

Participants

Reaction Steps

Mix 1-methyl-4-(N-(2-fluoro-3-bromophenyl)methylamino)piperidine (Preparation 24, 0.42 g), benzophenone imine (0.303 g), Pd2(dba)3 (25 mg), racemic BINAP (35 mg) and sodium t-butoxide (0.187 g) in toluene (10 mL) and heat at reflux for 3 hours. Dilute the reaction mixture with methanol (5 mL), load on a SCX column (10 g), wash with methanol, elute the with 2M NH3 in methanol, evaporate and further purify on a silica gel column (10 g), using a gradient of dichloromethane-2M NH3 in methanol to give 0.44 g of the title intermediate.

Provenance & Evidence