Chirality and Crop Protection

Chirality and Crop Protection
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DOI:
10.1002/anie.199111933
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发表时间:
1991-10
期刊:
影响因子:
--
通讯作者:
G. R. Tombo;D. Belluš
G. R. Tombo;D. Belluš
中科院分区:
--
文献类型:
--
作者:
G. R. Tombo;D. Belluš

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现代农业化学工业正在比以往任何时候都更加密集地寻找新的物质来对抗害虫(杂草、有害昆虫、植物病原体等)。在复杂而昂贵的选择和优化过程中,总是需要最先进的科学方法。跨学科优化的目标主要是降低新物质的应用率,增加对目标生物的选择性,以及优化生态概况。如果有前途的作物保护化合物是外消旋体或非对映异构体混合物,化学家就有独特的机会通过合成对映异构体纯的异构体来促进这一优化过程。如果单一异构体证明在生物学上上级外消旋体,那么开发一种经济和生态上无害的单一异构体生产工艺将是一个更大的挑战。作物保护化合物的平均价格比药物产品的平均价格低得多,这一事实严重限制了从事立体化学纯农用化学品的合成和生产的化学家的灵活性。这迫使作物保护化学家充分利用他的科学和创造能力。幸运的是,与现代和生态上合理的作物保护研究的上述优化目标的发展平行,在不对称合成领域也取得了持续的世界性进展。由于这两种平行努力的相互作用,近年来化学、生物学和农学知识有了很大的积累,其影响应该超出对映体纯农用化学品的合成。
The modern agrochemical industry is searching, more intensively than ever, for new substances to combat pests (weeds, deleterious insects, plant pathogens, etc.). In the complex and costly selection and optimization process, state-of-the-art scientific methods are always needed. The aims of the interdisciplinary optimization are mainly the reduction of the rate of application of the new substance, an increase in the selectivity against the target organism, and the optimal ecological profile. If a promising crop protection compound is a racemate or a diastereoisomeric mixture, the chemist has a unique opportunity to contribute to this optimization process through the synthesis of enantiomerically pure isomers for testing purposes. If the single isomer proves to be biologically superior to the racemate, the development of an economical and ecologically sound process for the production of the single isomer presents an even greater challenge. The average price of a crop protection compound is much lower than that for a pharmaceutical product, and this fact imposes a severe limitation upon the flexibility of the chemist who is concerned with the synthesis and production of a stereochemically pure agrochemical. This forces the crop protection chemist to make full use of both his scientific and creative capabilities. Fortunately, parallel to the development of the above optimization aims of a modern and ecologically sound crop protection research, there has been a continuous and worldwide advance in the area of asymmetric synthesis. Due to the interplay of these two parallel efforts there has been a great accumulation of chemical, biological, and agronomical knowledge in recent years, which should have implications beyond merely the synthesis of enantiomerically pure agrochemicals.