Triphenylphosphine → 4-Chloro-N-(6-methoxy-pyridin-3-ylmethyl)-N-((R)-2-oxo-azepan-3-yl)-benzenesulfonamide

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Reaction Steps

4-Chloro-N-((R)-2-oxo-azepan-3-yl)-benzenesulfonamide (0.04 g, 0.12 mmol), (5-Methoxy-pyridin-2-yl)-methanol (0.04 g, 030 mmol), triphenyl phosphine (0.08 g, 0.30 mmol) were dissolved in dry CH2Cl2 (6 ml) under an argon atmosphere followed by the dropwise addition of diisopropyl azodicarboxylate (60 mg, 0.30 ml) in dry CH2Cl2 (2 ml). The reaction mixture was further stirred overnight at r.t. and then concentrated under reduced pressure. The crude yellow oil was purified over silica gel (ethyl acetate/n-heptane 3:2): colorless gum 0.23 g (43%); MS: m/e=424.0 (MH+), 446.0 (MNa+).

Provenance & Evidence