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. 2018 Sep 12;9(11):1082–1087. doi: 10.1021/acsmedchemlett.8b00305

Scheme 1. Synthesis of Spiropiperidine Analog 10.

Scheme 1

Reagents and conditions: (a) K3PO4, Pd2(dba)3, dioxane, 100 °C, 88%; (b) HCl, dioxane, EtOAc, RT, 95%; (c) Cs2CO3, DMF, RT, 86%; (d) LiOH, MeOH, 50 °C, 79%. For synthesis of intermediate 14, see Supporting Information.