Binap, (A+-)- → 5-Chloro-6-(4-[2-(3-chloro-4-fluoro-phenyl)-6-morpholin-4-yl-pyridin-4-yl]-piperazin-1-yl}-nicotinic acid ethyl ester

Participants

Reaction Conditions

Reaction Steps

To a de-gassed mixture of 4-{4-bromo-6-(3-chloro-4-fluoro-phenyl)-pyridin-2yl}-morpholine (50 mg, 0.135 mmol), 5-chloro-6-piperazin-1-yl-nicotinic acid ethyl ester (0.162 mmol), and 1M (THF) t-BuOK (0.162 mmol), in toluene (3 mL) under nitrogen add Pd2(dba)3 (0.0054 mmol) and BINAP (0.0067 mmol). Stir the mixture at 80° C. for 16 h, concentrate, extract with EtOAc. Dry over Na2SO4, concentrate under vacuum, and purify by preparative TLC (3:1 hexanes/EtOAc) to give the title compound.

Provenance & Evidence