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Outline of synthetic routes to PAT analogues 5 and 6. Reagents and conditions: (i) 2% H2NNH2⋅H2O in DMF, 25 °C, 30 min, 91%; (ii) HBTU, iPr2NEt, DMF, 0 °C, 5 min then 25 °C, 30 min, 78% (54), 57% (62) and 64% (56); (iii) 25% Et2NH in CH2Cl2, 25 °C, 1 h, 90% (55); (iv) PhSH/Na2CO3, DMF, 25 °C, 12 h, 72% (57) and 65% (61); (v) 50% TFA in CH2Cl2, PhSH, 25 °C, 1 h, 87% (5) and 90% (9).
