Triphenylphosphine → (2E,4R)-5-(1,1'-Biphenyl)-4-yl-4-(((1,1-dimethylethoxy)carbonyl)amino)-2-methyl-2-pentenoic acid

Participants

Reaction Steps

A mixture of (R)-5-Biphenyl-4-yl-4-tert-butoxycarbonylamino-2-methylenepentanoic acid (0.38 g, 1 mmol, Example 32 in WO 2009/090251), Pd(PPh3)4 (70 mg, 0.06 mmol), PPh3 (31.5 mg, 0.12 mmol) and sodium bicarbonate (0.27 g, 3.2 mmol) in 10 mL xylene is heated to reflux, and stirred overnight to afford (R)-5-Biphenyl-4-yl-4-tert-butoxycarbonylamino-2-methyl-pent-(E)-2-enoic acid as determined by HPLC analysis. Spectroscopic data as reported in Example 1 in WO 2008/031567.

Provenance & Evidence