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. 2019 Jan 30;166:328–338. doi: 10.1016/j.ejmech.2019.01.074

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Scheme 1 — Reagents and conditions: (a) TBTU, DIPEA, THF, 90%; (b) Na₂CO₃, R—NH₂, DMF, 60 °C, 46–82%; (c) TsCl, NaOH, H₂O, 11%; (d) NaN₃, DMF, 80 °C, 81%; (e) Ac₂O, pyridine, DMAP, 86% for 16, or NaH, CH₃I, DMF, 62% for 17; (f) sodium l-ascorbate, CuSO₄, THF-H₂O (1:1, v/v), 45–61%; (g) CH₃ONa/CH₃OH, 80–98%.