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. 2021 Jun 29;12(8):1245–1252. doi: 10.1021/acsmedchemlett.1c00032

Scheme 3. Synthesis of Spirocyclic Thiohydantoin Analogue 16 and Phenol Metabolite 17.

Scheme 3

Reagents and conditions: (a) Pd(dppf)Cl2, KOAc, 1,4-dioxane, 80 °C; (b) oxone, acetone, rt; (c) TFA, DCM, rt; (d) TEA, THF, DMF, 80 °C; (e) DEAD, PPh3, THF, 60 °C; (f) HCl, 1,4-dioxane, rt.