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. 2022 Mar 10;13(4):593–598. doi: 10.1021/acsmedchemlett.1c00652

Scheme 1. Synthetic Route for Compounds 2–10.

Scheme 1

Reagents and conditions: (a) Oxone, MeOH, rt, 4 h, 86%; (b) KNO3, conc. H2SO4, 90 °C, 3 h, 80%; (c) oxyl chloride, DCM, then KNCS; (d) intermediates 33a–33e, yield 32%–55%; (e) 1-Boc-piperazine, NaBH3CN, rt, DCM, 88–93%; (f) CF3COOH, DCM, rt.