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. Author manuscript; available in PMC: 2020 Dec 11.
Published in final edited form as: J Med Chem. 2020 Jun 18;63(13):7033–7051. doi: 10.1021/acs.jmedchem.0c00366

Scheme 2. Synthesis of 4–9α.

Scheme 2.

αReagents and conditions: (a) 4: Troc-Cl, DIPEA, DMAP, DCM, 40 °C, 12 h, N2, 95 °C, 10h. 5: TEA, DCM, CDI, 0–20 °C, 14 h. 6,7: TEA, DCM, CDI, 5–10 °C, 3 h, 10–15 °C, 12 h. 8: Troc-Cl, DIEA, DCM, 0–20 °C, 1 h, DMF, 90 °C, 12h; 9: TEA, DCM, CDI, 5–10 °C, 3 h, 10–15 °C, 2 h;