HCID 10637170, compound → HCID 10648298, compound

Participants

Reaction Steps

A solution of (E)-3-[4-(4-oxo-piperidin-1-yl)-phenyl]-acrylic acid (which was obtained in Example 170) (0.10 g, 0.40 mmol) and N-[5-((1R)-2-Amino-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methane-sulfonamide (which was obtained in Example 10) (0.12 g, 0.48 mmol) in methanol (15 mL) was treated with avetic acid (0.03 g, 0.5 mmol), and 0.05 g of 10% Pd/C. The mixture was hydrogenated at 25 psi for 24 h, and then filtered through Celite and evaporated. The residue was triturated with ether to give 0.18 g of an off-white solid; m.p. 130–133° C.; 1H NMR (DMSO-d6) δ 1.30–1.46 (m, 2 H), 1.84–1.95 (m, 2 H), 2.37–2.50 (m, 4 H), 2.60–2.78 (m, 4 H), 2.92 (s, 3 H), 3.53–3.62 (m, 3 H), 4.46–4.55 (m, 1 H), 6.85 (d, 2 H), 6.92–7.10 (m, 4 H), 7.18 (dd, 1 H); MS (ES) m/z: 478.3 (MH+).

Provenance & Evidence