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. Author manuscript; available in PMC: 2020 Oct 13.
Published in final edited form as: Bioorg Med Chem Lett. 2009 Nov 12;20(2):763–766. doi: 10.1016/j.bmcl.2009.11.018

Scheme 1.

Scheme 1.

Typical synthetic route of spirodiketopiperazines. Reagents and conditions: (a) MeOH, 55 °C; (b) concd HCl, 55 °C; (c) AcOH, toluene, 80 °C; (d) H2, Pd(OH)2/C, EtOH, 55 °C then 4 N HCl/AcOEt (60–70% in four steps); (e) Ar-CHO, NaBH(OAc)3, AcOH, DMF, then 4 N HCl/AcOEt (50–90%).