Beijing National Laboratory for Molecular Sciences (BNLMS), CAS Key Laboratory of Molecular Recognition and Function, CAS Research/Education Center for Excellence in Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
Molecules. 2023 Apr 25;28(9):3715. doi: 10.3390/molecules28093715.
Cyclooctyne molecules have found wide applications in the strain-promoted azide-alkyne cycloaddition (SPAAC) reactions, which avoid the biotoxicity caused by the use of Cu(I) catalysts. Among the various cyclooctyne systems, dibenzocyclooctyne (DBCO) series have displayed the highest reaction activity. However, the synthesis processes of such structures are time-consuming, which to some extent limit their large-scale development and application. This review has summarized current synthesis routes of two DBCO molecules, aza-dibenzocyclooctyne (DIBAC) and biarylazacyclooctynone (BARAC).
环辛炔分子在应变促进的叠氮-炔环加成（SPAAC）反应中得到了广泛的应用，该反应避免了使用 Cu(I)催化剂所带来的生物毒性。在各种环辛炔体系中，二苯并环辛炔（DBCO）系列显示出最高的反应活性。然而，此类结构的合成过程耗时较长，在一定程度上限制了它们的大规模发展和应用。本文综述了两种 DBCO 分子，氮杂二苯并环辛炔（DIBAC）和双芳基氮杂环辛炔酮（BARAC）的现有合成路线。
