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

Scheme 1. Synthesis of Spirocyclic Thiohydantoin Analogues 1822 and 2629.

Scheme 1

Reagents and conditions: (a) NBS, AIBN (cat), CCl4, 85 °C; (b) K2CO3, 18-crown-6, MeCN, rt; (c) aq. HCl, rt; (d) NaBH(OAc)3, DCE, rt; (e) TEA, THF/DMF, 80 °C; (f) MeNH2·HCl (or MeNHOMe·HCl), W(CO)6 (cat.), Pd(OAc)2 (cat.), Xantphos (cat.), TEA, 1,4-dioxane, 80 °C; (g) SFC chiral separation.