Preparation method of trifluoromethyl sulfide aza-8/9-membered ring compound

• Main Authors: ALI, AYMUNISA, TANG JUNHONG, ZHU YARU, SUN KAI, ZHANG ZHEN, CHEN JINCHUN, FANG XIANGSHAN, LIN WANJUN
• Format: Patent
• Language: Chinese; English
• Published: 21.11.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a preparation method of a trifluoromethyl sulfide aza-8/9-membered ring compound, which is characterized in that a modifiable diene substrate and AgSCF3 are subjected to a tandem cyclization reaction under the action of K2S2O8 and HMPA to obtain a target product in one step. The used substrate can selectively realize the synthesis of 8-membered and 9-membered trifluoromethylsulphide nitrogen heterocyclic rings by prolonging a carbon chain. The invention provides a novel preparation technical route. The reaction process involved in the preparation method is simple, the conditions are mild, strict anhydrous and anaerobic conditions are not needed, and the operability is high; the substrate is high in universality, and the potential of large-scale application is relatively high. 本说明公开了一种三氟甲硫化氮杂-8/9元环化合物的制备方法，可修饰的二烯底物与AgSCF3，在K2S2O8和HMPA的作用下发生串联环化反应，一步得到目标产物。所用的底物可通过延长碳链，选择性实现8元和9元三氟甲硫化氮杂环的合成。本发明提供了一种新的制备技术路线。而且本发明制备方法所涉及的反应过程简洁，条件温和，不需要严格的无水无氧条件，可操作性强；底物普适性高，规模化应用的潜力较高。