The copper (I) catalyzed cycloaddition reaction of N-Boc propargyl amine (dipolarophile) 1 with benzyl azide (1, 3-dipole) 2 was found to proceed smoothly in t-BuOH/H2O at room temperature, to furnish the corresponding 1, 4-disubstituted-[1, 2, 3]-triazole-derived N-Boc amine 3 in good yield. Deprotection of 3 with trifluoroacetic acid and addition of the trifluoroacetate salt 4 in the presence of triethylamine, with a series of methoxyvinyl ( ...
