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. 2020 Apr 18;10(12):2339–2347. doi: 10.1016/j.apsb.2020.04.003

Scheme 2.

Scheme 2

The general synthetic route summarized for the preparation of the compounds 114. Reagents and conditions: (a) methyl acrylate, NaOCH3, methanol, reflux, 4 h; (b) methyl acrylate, TEA, (PPh3)2PdCl2, N,N-dimethylformamide, Ar, 120 °C, overnight; (c) Pd/C, H2, ethanol, room temperature, overnight; (d) 6 mol/L NaOH, ethanol, room temperature, overnight; (e) i) 2-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (HATU), N,N-diisopropylethylamine (DIPEA), CH2Cl2, overnight; ii) acetic acid, 90 °C, overnight.