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Outline of synthetic route to PhTX-433 analog 8. Reagents and conditions: (i) PhthN(CH2)4Br, K2CO3, DMF, 60 °C, 2.5 h; (ii) H2NNH2.H2O, EtOH, 80 °C, 1 h, 52%; (iii) HBTU, iPr2NEt, DMF, 0 °C, 5 min then 25 °C, 30 min, 60% (69); (iv) 25% Et2NH in CH2Cl2, 25 °C, 1–2 h; (v) PhSH/Na2CO3, DMF, 25 °C, 12 h, 74%; (vi) 50% TFA in CH2Cl2, PhSH, 25 °C, 1 h, 83%.
