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Andrew R. Bogdan and Keith James Efficient Access to New Chemical Space Through Flow—Construction of Druglike Macrocycles Through Copper-Surface-Catalyzed Azide–Alkyne Cycloaddition Reactions Chemistry - A European Journal 16

Version of Record online: 29 OCT 2010 | DOI: 10.1002/chem.201002215

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Making macrocycles on the move! A series of 12- to 22-membered macrocycles with druglike functionality and properties have been generated by using the copper-catalyzed azide–acetylene cycloaddition reaction, conducted in flow in high-temperature copper tubing. The triazole-containing macrocycles have been generated in up to 90 % yield in a 5 min reaction, without resorting to high-dilution conditions.

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