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. 2011 Mar 11;2(5):402–406. doi: 10.1021/ml200045s

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Scheme 2 — Conditions: (a) 2,5-dimethoxytetrahydrofuran/AcOH. (b) POCl₃/DMF. (c) Ph₃P = CHCO₂Et, toluene, reflux. (d) potassium 3-ethoxy-3-oxopropanoate, DMAP/piperidine/AcOH/DMF, 80 °C. (e) H₂, 10% Pd/C in EtOH. (f) NBS. (g) boronic acid, Pd(PPh₃)₄, Na₂CO₃. (h) K₂CO₃, H₂O₂/DMSO, room temperature. (i) LiOH.