Scheme 1.
Synthesis of cinnamoyl triazole derivatives 8a–h and 9a–h. Reagents, conditions, yield: i = SOCl2, DMFcat, reflux 3 h then N3EtOH, pyridine/CH2Cl2, rt overnight, 72%, or (COCl2), DMFcat, CH2Cl2, 0°C 3 h then N3EtNH2, pyridine/CH2Cl2, rt overnight, 70%. ii = HCCH, CuI, NEt3, DMSO, rt overnight, 68–88%, or R1CCH, CuI, NEt3, THF, rt overnight, 11–83%.