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. 2017 Sep 29;8(10):1060–1065. doi: 10.1021/acsmedchemlett.7b00269

Scheme 2. Synthesis of Ester Derivatives 13a–e.

Scheme 2

Reagents and conditions: (a) H2, Pd/C, MeOH, rt, 35–60 min; (b) Boc2O, Et3N, DMF, rt, 1–2.5 h; (c) benzyl alcohol or substituted benzyl alcohol, DCC, DMAP, DMF, rt, 3.5 h–overnight, 43–82% (3 steps); (d) 4 M HCl/dioxane, rt, 1 h, then RP-HPLC purification, 23–55%. R4 substituents of derivatives 13a–e are shown in Table 2.