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Synthesis of analogues with different core motifs. Reagents and conditions: (a) 1-Boc-pyrazole-4-boronic acid pinacol ester, cat. PdCl2(PPh3)2, 1 M Na2CO3(aq)/THF, 100 °C, 28%; (b) TFA, DCM, rt, 46%; (c) (bromomethyl)cyclopentane, K2CO3, DMF, rt-60 °C, 55%; (d) pinacol ester, cat. PdCl2(PPh3)2, Cs2CO3, DMF or DME, 100 °C, 16–63%; (e) pinacol ester, cat. PdCl2(PPh3)2, 1 M Na2CO3(aq)/THF, 100 °C, 7–8%.
