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Preparation of Enantiopure Non-Activated Aziridines and Synthesis of Biemamide B, D, and epiallo-Isomuscarine
Published on: June 13, 2022
Synthesis of Maleimide Derivatives and Benzo[1,4]oxetane Derivatives: a Modification Method of Amine-Containing
Lu Yin1, Meitian Fu1, Sihan Zhao1
1Key Laboratory of Biomass Green Chemical Conversion of Yunnan Provincial Education Department, Yunnan Key Laboratory of Chiral Functional Substance Research and Application, School of Chemistry & Environment, Yunnan Minzu University, Kunming 650504, PR China.
Abstract:
Maleimide-modified drug molecules can improve the stability and selective release of drugs. This study developed an easy-to-operate, mild, and safe synthetic drug-molecule modification strategy. This strategy employs the easily substituted characteristics of the substrate aminomaleimide and various amine-containing molecules under catalyst-free conditions. This method is suitable for various types of primary amines and secondary amines. When reacting with N-methylbenzylamine, benzo[1,4]oxazepane derivatives can be obtained by temperature adjustment. At the same time, the method has good tolerance for substrate functional groups, and 7 maleimide-modified drug molecular fragments were obtained in high yield (80-85%). This article has confirmed that the drug molecules modified by this method still have active reaction sites and can be further modified.
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