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. Author manuscript; available in PMC: 2020 Feb 14.
Published in final edited form as: J Med Chem. 2019 Feb 5;62(3):1643–1656. doi: 10.1021/acs.jmedchem.8b01958

Scheme 3. Synthesis of 8–12a.

Scheme 3.

aReagents and conditions: (a) 4N HCl in 1,4-dioxane, CH2Cl2, rt then R1–NH2, phenylchlorothionoformate, iPr2NEt3, CH2Cl2, 21–45 %; (b) 4N HCl in 1,4-dioxane, CH2Cl2, rt then R1–N=C=S or R1–N=C=O, iPr2NEt3, CH2Cl2, rt, 71–100 %.