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Route Evaluation and Ritter Reaction Based Synthesis of Oxazoline Acaricide Candidates FET-II-L and NK-12

Yu Zhang, Shilin Chen, Yuxiu Liu, Qingmin Wang

2020Organic Process Research & Development18 citationsDOI

Abstract

Clean synthetic processes are essential for industrial production of bioactive molecules. In this study, we explored several routes for the synthesis of acaricide candidates FET-II-L and NK-12 with the goal of developing a rapid route that is suitable for industrial production. Our results led us to adopt a Ritter reaction based aminohalogenation strategy that features fewer steps, simpler operation, and greatly increased overall yields relative to those of previously reported syntheses. After further optimization, the route reported herein is likely to be applicable for large scale production of these molecules.

Topics & Concepts

Ritter reactionAcaricideCombinatorial chemistryChemistryOxazolineOrganic chemistryCatalysisSynthesis and Biological EvaluationChemical Synthesis and ReactionsOxidative Organic Chemistry Reactions
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