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. Author manuscript; available in PMC: 2018 Mar 10.
Published in final edited form as: Eur J Med Chem. 2017 Jan 30;128:168–179. doi: 10.1016/j.ejmech.2017.01.041

Scheme 1a. Synthesis of HPD subtype 4.

Scheme 1a

aReagents and conditions: a) CDI, CH3CN, rt, 30 min, R1CH(CO2Et)(CO2K), Et3N–MgCl2, rt, overnight; b) Zn, THF; c) thiourea, EtONa, EtOH, refluxing for 8h; d) ClCH2COOH, AcOH, H2O, refluxing, overnight; e) CH3C(OTMS)=NTMS (BSA), substituted benzyl alcohol, (HCHO)n, TMSCl, TBAI ( cat.), CH2Cl2, rt, 70–90%; f) NaH, mCPBA, THF, rt.