A Green Method For The Preparation Of Phoxim Based On High-Boiling Nitrite

Changzan Dong, Jinwen Qiao, Hongwei Zhu,Guang Qian,Jie Zhu,Yupeng He

GREEN PROCESSING AND SYNTHESIS(2021)

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摘要
Phoxim is a significant insecticide, and its current synthesis method has some shortcomings such as the high risk of explosion and the trans structure (main impurity) is hard to control. Our work solved the above disadvantages by introducing macromolecular alcohol (benzyl alcohol, etc.) as the starting material and optimizing the intermediate reaction conditions. Compared with the current synthesis route, the synthetic method has the following advantages: (1) intermediate benzyl nitrite has a high boiling point and strong safety; (2) intermediate alpha-cyanobenzaldehyde oxime sodium are almost (>= 99%) cis structure, and no further refinement was required, which greatly reduced the amount of waste water produced; and (3) The high yield of phoxim was maintained at 72.9%.
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关键词
benzyl alcohol, phoxim, alpha-cyanobenzaldehyde, oxime sodium, drug synthesis
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