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Synthesis of PZQ analogues 1–22.
Reagents and conditions: (a) 2 N HCl, reflux, overnight, 62%; (b) TFAA, Et3N, DCM, 62% or RCOCl, Et3N, DCM, 29%–50%; (c) RCHO, NaBH4, HOAc, MeOH, 0 °C to 60 °C, 27%–35%; (d) LiAlH4, THF, 0 °C, 35%; (e) RCOCl, Et3N, DCM, 32%–69%.
