Tributylphosphine → Ethyl 3-[2,6-difluoro-4-[[4-[[(2-phenylethyl)(4-phenyl-1,3-thiazol-2-yl)amino]methyl]benzyl]oxy]phenyl]-propanoate

Participants

Reaction Steps

That is, to a solution of [4-[[(2-phenylethyl)(4-phenyl-1,3-thiazol-2-yl)amino]methyl]phenyl]methanol (350 mg, 0.87 mmol), ethyl 3-(2,6-difluoro-4-hydroxyphenyl)propanoate (200 mg, 0.87 mmol) and tributylphosphine (0.31 mL, 1.24 mmol) in tetrahydrofuran (30 mL) was added 1,1′-(azodicarbonyl)dipiperidine (320 mg, 1.27 mmol), and the mixture was stirred at room temperature for 18 hr. The insoluble materials were filtered off and the filtrate was concentrated. The residue was purified by silica gel column chromatography to give the title compound (300 mg, yield 56%) as a colorless oil.

Provenance & Evidence