Scheme 2.
a(i) NaOH, NH2OH·HCl, tBuOH/H2O (1:1), then TsN(Cl)Na·H2O, then CuSO4·5H2O, NaHCO3, 1-chloro-3-ethynylbenzene (ii) F3CCO2H, CH2Cl2 (iii) MeN=C=S, CH2Cl2 (iv) NaOtBu, THF, MeI (v) iPrOH, pyridine, microwave, 150 °C, 2 h., 6%
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