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. 2021 Oct 5;12(11):1802–1809. doi: 10.1021/acsmedchemlett.1c00416

Scheme 2.

Scheme 2

Reagents and conditions: (a) H2SO4, NaNO2, 0 °C to rt, 16 h; (b) HATU, TEA, DCM, rt, 16 h; (c) I2, HMDS, DCM, 50 °C, 16 h; (d) TBAF, THF, 0 °C, 30 min; (e) 2,6-lutidine, Tf2O, DCM, −78 °C, 2 h; (f) DMF/DCM, −78 °C to rt, 4 h (; (g) MsCl, DIPEA, DCM, −78 °C, 5 min; (h) ACN, 80 °C, 24 h.