三氟甲基化
芳基
三氟甲基
塞流
基质(水族馆)
期限(时间)
组合化学
化学
计算机科学
有机化学
物理
热力学
生物
生态学
量子力学
烷基
作者
Rajaram Ayothiraman,Aravind S. Gangu,Durgarao Bandaru,Siva Krishna Guturi,Thirumalai Lakshminarasimhan,Mohamed Jaleel,Kishorekumar Kanagavel,Sundaramurthy Rangaswamy,Nicolas Cunière,Serge Zaretsky,Kathryn M. Camacho,Martin D. Eastgate,Rajappa Vaidyanathan
标识
DOI:10.1021/acs.oprd.9b00492
摘要
Two approaches to a 1-aryl-4-trifluoromethyltriazole are described. Initially, a late-stage trifluoromethylation of the corresponding 1-aryl-4-iodotriazole using methyl fluorosulfonyldifluoroacetate (MDFA) was employed. However, the reaction was fraught with several safety and operational challenges, primarily due to the evolution of ∼33 equiv of gas per equiv of substrate. While some of these challenges were either addressed or mitigated through operations in plug flow, the process remained low yielding and suboptimal. Subsequently, a more convergent, longer-term route involving a Cu-mediated decarboxylative Click reaction was developed.
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