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. 2020 Dec 9;12(1):88–92. doi: 10.1021/acsmedchemlett.0c00485

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© 2020 American Chemical Society

This article is made available via the ACS COVID-19 subset for unrestricted RESEARCH re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for the duration of the World Health Organization (WHO) declaration of COVID-19 as a global pandemic.

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Scheme 2 — Reagents and conditions: (a) DBDC, Na₂CO₃, dioxane/H₂O, 35% for 13a, 23% for 13b, and 59% for 13c; (b) phenyl dichlorophosphate, triethylamine, CH₂Cl₂, −78 °C, quantitative yield; (c) tert-butylmagnesium chloride, anhydrous THF; (d) trifluoroacetic acid/CH₂Cl₂, 0 °C, 49% for 16a, 54% for 16b, and 32% for 16c.