State Key Laboratory of Natural Medicines (SKLNM) and Department of Medicinal Chemistry, School of Pharmacy , China Pharmaceutical University , Nanjing 210009 , P. R. China.
Org Lett. 2018 Apr 6;20(7):1781-1784. doi: 10.1021/acs.orglett.8b00280. Epub 2018 Mar 20.
A formal [3 + 3] cycloaddition reaction between azides and in situ formed azaoxyallyl cations has been realized. This reaction provided an efficient and practical pathway to synthesize 1,2,3,4-tetrazines in good yields under mild conditions. Biologically active molecules could also be well compatible, highlighting the potential value of this reaction.
已实现叠氮化物和原位形成的氮杂氧杂烯丙基阳离子之间的[3 + 3]环加成反应。该反应在温和条件下以良好的收率提供了一种有效且实用的方法来合成 1,2,3,4-四嗪。生物活性分子也能很好地兼容,突出了该反应的潜在价值。