Route Evaluation and Ritter Reaction Based Synthesis of Oxazoline Acaricide Candidates FET-II-L and NK-12,Organic Process Research & Development

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Route Evaluation and Ritter Reaction Based Synthesis of Oxazoline Acaricide Candidates FET-II-L and NK-12
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-02-10 , DOI: 10.1021/acs.oprd.9b00494
Yu Zhang ₁ , Shilin Chen ₁ , Yuxiu Liu ₁ , Qingmin Wang _{1,

2}

Affiliation

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.

中文翻译：

路线评估和基于Ritter反应的恶唑啉类杀螨剂FET-II-L和NK-12的合成

清洁合成工艺对于生物活性分子的工业生产至关重要。在这项研究中，我们探索了几种合成候选杀螨剂FET-II-L和NK-12的途径，目的是开发一种适合工业生产的快速途径。我们的结果使我们采用了基于Ritter反应的氨基卤化策略，与以前报道的合成方法相比，该方法具有更少的步骤，更简单的操作并大大提高了总产率。在进一步优化之后，本文报道的途径可能适用于这些分子的大规模生产。

更新日期：2020-02-10

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