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Amine-catalyzed [3+2] Huisgen cycloaddition strategy for the efficient assembly of highly substituted 1,2,3-triazoles

机译:胺催化的[3 + 2] Huisgen环加成策略可有效组装高度取代的1,2,3-三唑

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摘要

An enamine-catalyzed strategy has been utilized to fully promote the Huisgen [3+2] cycloaddition with a broad spectrum of carbonyl compounds and azides, thereby permitting the efficient assembly of a vast pool of highly substituted 1,2,3-triazoles. In particular, the employment of commonly used and commercially available carbonyl compounds has resulted in the introduction of a diverse set of functional groups, such as alkyl, aryl, nitrile, ester, and ketone groups, at the 1-, 4-, or 5-positions of the 1,2,3-triazole scaffold. This approach might be manipulated to access more useful and sophisticated heterocyclic compounds. Most significantly, the reaction process exhibits complete regioselectivity, with the formation of only one regioisomer.
机译:烯胺催化的策略已被用来充分促进具有宽范围的羰基化合物和叠氮化物的Huisgen [3 + 2]环加成反应,从而可以有效地组装大量高度取代的1,2,3-三唑。尤其是,使用常用的和可商购的羰基化合物导致在1-,4-或5处引入了多种官能团,例如烷基,芳基,腈,酯和酮基。 1,2,3-三唑支架的-位。可以使用此方法来访问更有用和更复杂的杂环化合物。最重要的是,反应过程表现出完全的区域选择性,仅形成一种区域异构体。

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