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《农业科学与工程前沿(英文)》 doi: 10.15302/J-FASE-2021390

ROUTE DEVELOPMENT, ANTIVIRAL STUDIES, FIELD EVALUATION AND TOXICITY OF AN ANTIVIRAL PLANT PROTECTANT NK0238

. State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China... Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300071, China.

收稿日期 :2021-03-26 录用日期 : 2021-04-26 发布日期 :2021-04-26

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摘要

It has previously been shown that tryptophan, the biosynthesis precursor of alkaloids, and its derivatives have anti-TMV activity both and . Further exploration of this led to the identification of NK0238 as a highly effective agent for the prevention and control of diseases caused by plant viruses, but the existing routes are unsuitable for its large-scale synthesis. This study optimized a route for two-step synthesis of this virucide candidate via reaction of L-tryptophan with triphosgene to produce L-tryptophan- -carboxylic anhydride, which then reacts with -octylamine to give NK0238 at up to 94% yield and nearly 97% HPLC purity. In addition, the route was used for the preparation of NK0238 on a > 40 g scale permitting further assessment of its antivirus activity in the greenhouse and field experiments, and toxicity tests. NK0238 exhibited useful antiviral activities against a variety of viruses both in greenhouse and field experiments. The toxicity tests showed that NK0238 was not acutely toxic to birds, fish, honey bees and silkworms. The optimized route provides a solid foundation for its large-scale synthesis and subsequent efficacy and toxicity studies, its excellent activity and safety make NK0238 a promising drug candidate for further development.

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