Triethylamine → (RS)-N-(4-cyano-benzyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-2-methoxy-acetamide

Participants

Reaction Steps

To a solution of (RS)-N-(4-cyano-benzyl)-2-(2,6-difluoro-3-hydroxy-phenyl)-2-methoxy-acetamide (370 mg) in 1,2-dichloroethane (10 ml) was added copper(II)acetate (222 mg), 4-fluorobenzoic acid (467 mg) and powdered MS4 Å (2 g). Et3N (563 mg) was added and the mixture was stirred 2 days at rt. The mixture was passed over silica gel eluting with AcOEt. CC (AcOEt/Hept 1:3 to 3:1) yielded 203 mg (61%) of (RS)-N-(4-cyano-benzyl)-2-[2,6-difluoro-3-(4-fluoro-phenoxy)-phenyl]-2-methoxy-acetamide. Yellow oil. MS 427.0 ([M+H]+).

Provenance & Evidence