新农药创新方法与应用(1)—中间体衍生化方法

New Approach for Agrochemical Discovery and Application(1)——Intermediate Derivatization Method

介绍了一种发现新农药的创新研究方法——中间体衍生化方法。新农药创新涉及多领域间的合作,其过程非常复杂,中间体衍生化方法是从化学的角度出发,把复杂问题简单化,应用效果很好。通过多年的实践,总结其内涵有三:利用中间体进行化学反应,设计合成新化合物,然后筛选,发现先导化合物,再经优化发现新农药品种;利用简单的原料,通过化学反应合成新的中间体,利用该中间体替换已知农药或医药品种化学结构中的一部分,得到新的化合物,经进一步研究,得到新农药品种;利用已知的具有活性的化合物或农药品种作为中间体,进行化学反应,设计合成新化合物,经筛选、优化研究发现新农药品种。

A new discovery approach in R＆D of novel agrochemicals（crop protection products）, intermediate derivatization method, was introduced. New agrochemical R＆D is a very complicated process concerning multi-discipline research. Intermediate derivatization method can simplify the complicated matters from the perspective of chemistry and the application effect is very significant. Three connotation was summarized through many years of practice： design, synthesize new compounds by chemical reaction utilizing various intermediates, screen and discover lead compounds, and then discover new agrochemicals after optimization. New intermediates were synthesized through chemical reaction by using some raw materials, and use them to replace the parts of chemical structures of the known agrochemicals or pharmaceuticals to obtain new lead compounds which were further researched for new products. Design and synthesize new compounds via chemical reaction using the known and active compounds or agrochemicals as intermediates, and then screen and optimize to find new crop protection products.