Trimethyl phosphite → (R)-ethyl 4-(4-((4'-chlorobiphenyl-2-yl)(dimethoxyphosphoryloxy)methyl)piperidin-1-yl)benzoate

Participants

Reaction Steps

A similar procedure to that described for INTERMEDIATE 119 utilizing (R)-ethyl 4-(4-((4′-chlorobiphenyl-2-yl)(hydroxy)methyl)piperidin-1-yl)benzoate (INTERMEDIATE 11A, 600 mg, 1.33 mmol) and trimethyl phosphite (0.473 ml, 4.0 mmol) as starting material was followed, with subsequent purification by column chromatography (ISCO, 0→100% EtOAc/hexane over 24 minutes) to give the title compound (500 mg, yield: 67%). The title compound was used in the preparation of INTERMEDIATE 122 without further purification.

Provenance & Evidence