Tributylphosphine → 4-{4-[3-(2-Chloro-3,6-difluoro-phenyl)-isoxazol-5-ylmethoxy]-phenyl}-5,6-dihydro-2H-pyridine-1,3-dicarboxylic Acid 1-tert-butyl Ester 3-methyl Ester

Participants

Reaction Conditions

Reaction Steps

To a sol. of compound B2 (10.0 g, 30 mmol) and [3-(2-chloro-3,6-difluoro-phenyl)-isoxazol-5-yl]-methanol (8.84 g, 30 mmol) in toluene (60 mL) were added ADDP (15.1 g, 60 mmol) and PBu3 (90%, 30.0 mL; 108 mmol). The mixture was stirred for 2 h at 80° C., and was allowed to cool to rt. The solvents were removed under reduced pressure. Purification of the residue by FC (EtOAc/heptane 1:4→EtOAc) yielded the title compound (8.64 g, 51%). LC-MS: tR=1.15 min; ES+: 561.25.

Provenance & Evidence