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The Huisgen 1, 3-dipolar cycloaddition reaction of organic azides and alkynes1, 2 has gained considerable attention in recent years due to the introduction in 2001 of Cu (1) catalysis by Tornøe and Meldal, 3 leading to a major improvement in both rate and regioselectivity of the reaction, as realized independently by the Meldal and the Sharpless laboratories. 4, 5 The great success of the Cu (1) catalyzed reaction is rooted in the fact that it is a virtually quantitative, very robust, insensitive, general, and orthogonal ligation reaction, suitable for even biomolecular ligation6 and in vivo tagging7, 8 or as a polymerization reaction for synthesis of long linear polymers. 9 The triazole formed is essentially chemically inert to reactive conditions, eg oxidation, reduction, and hydrolysis, and has an intermediate polarity with a dipolar moment of∼ 5 D. 10 The basis for the unique properties and rate enhancement for triazole …