Synthesis process optimization and field trials of insecticide candidate NKY-312

Abstract NKY-312 is a highly active insecticide candidate with a simple structure. In order to carry out field trials and toxicity tests, its scale preparation is urgently needed, but the final step of the original synthetic route is a low-yielding sulfonylation reaction that generates a high propor...

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Autores principales:	Haiqi Wang, Hongjian Song
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/fb706e0f6a854ed59ec6de2e4cc034ea
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spelling	oai:doaj.org-article:fb706e0f6a854ed59ec6de2e4cc034ea2021-12-02T11:45:04ZSynthesis process optimization and field trials of insecticide candidate NKY-31210.1038/s41598-021-86475-w2045-2322https://doaj.org/article/fb706e0f6a854ed59ec6de2e4cc034ea2021-03-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-86475-whttps://doaj.org/toc/2045-2322Abstract NKY-312 is a highly active insecticide candidate with a simple structure. In order to carry out field trials and toxicity tests, its scale preparation is urgently needed, but the final step of the original synthetic route is a low-yielding sulfonylation reaction that generates a high proportion of a bissulfonylated by-product, its foliar contact activities against bean aphid (80% at 100 mg/kg) is significantly lower than that of NKY-312 (100% at 5 mg/kg), and uses pyridine as the solvent. In this work, we developed a highly selective (4-dimethylaminopyridine)-catalyzed monosulfonylation reaction that avoids the use of pyridine as a solvent and shows a much higher yield (98% yield with 98% HPLC purity) than the original reaction (68%). Then, we carried out the field trials and toxicity tests. In field experiments, the activities of NKY-312 against rice planthopper and wheat aphid were equal to pymetrozine and imidacloprid respectively.Haiqi WangHongjian SongNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-8 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Haiqi Wang Hongjian Song Synthesis process optimization and field trials of insecticide candidate NKY-312
description	Abstract NKY-312 is a highly active insecticide candidate with a simple structure. In order to carry out field trials and toxicity tests, its scale preparation is urgently needed, but the final step of the original synthetic route is a low-yielding sulfonylation reaction that generates a high proportion of a bissulfonylated by-product, its foliar contact activities against bean aphid (80% at 100 mg/kg) is significantly lower than that of NKY-312 (100% at 5 mg/kg), and uses pyridine as the solvent. In this work, we developed a highly selective (4-dimethylaminopyridine)-catalyzed monosulfonylation reaction that avoids the use of pyridine as a solvent and shows a much higher yield (98% yield with 98% HPLC purity) than the original reaction (68%). Then, we carried out the field trials and toxicity tests. In field experiments, the activities of NKY-312 against rice planthopper and wheat aphid were equal to pymetrozine and imidacloprid respectively.
format	article
author	Haiqi Wang Hongjian Song
author_facet	Haiqi Wang Hongjian Song
author_sort	Haiqi Wang
title	Synthesis process optimization and field trials of insecticide candidate NKY-312
title_short	Synthesis process optimization and field trials of insecticide candidate NKY-312
title_full	Synthesis process optimization and field trials of insecticide candidate NKY-312
title_fullStr	Synthesis process optimization and field trials of insecticide candidate NKY-312
title_full_unstemmed	Synthesis process optimization and field trials of insecticide candidate NKY-312
title_sort	synthesis process optimization and field trials of insecticide candidate nky-312
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/fb706e0f6a854ed59ec6de2e4cc034ea
work_keys_str_mv	AT haiqiwang synthesisprocessoptimizationandfieldtrialsofinsecticidecandidatenky312 AT hongjiansong synthesisprocessoptimizationandfieldtrialsofinsecticidecandidatenky312
_version_	1718395320415551488

Synthesis process optimization and field trials of insecticide candidate NKY-312

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