The beginning of chemical weeding can be traced back to the end of the 19th century. In the control of downy mildew of grape in Europe, Bordeaux solution was occasionally found to damage some cruciferous weeds without damaging cereal crops. In France, Germany and the United States, sulfuric acid and copper sulfate were also found for weeding and used for weeding in wheat and other fields. The period of organic chemical herbicide began with the discovery of dinitrophenol in 1932. The emergence of 2,4-drops in 1940s greatly promoted the rapid development of organic herbicide industry. Glyphosate, synthesized in 1971, has the characteristics of broad weed killing spectrum and no pollution to the environment. It is a major breakthrough of organophosphorus herbicides. In addition, the emergence of a variety of new dosage forms and new application technologies greatly improved the weeding effect. In 1980, herbicides accounted for 41% of the total sales of pesticides in the world, surpassing insecticides and ranking first.

There are o-isopropy-n-phe-nylcarbamate (IPC: c6h5nhcooch - (CH3) 2), sodium dinitro-o-cresylite, etc. The most famous herbicide with auxin function is 2,4-D, which is believed to disturb the hormone balance in plants and make physiological disorders, but it is a very effective herbicide for plants other than Gramineae. It is generally believed that the selectivity depends on the intensity of detoxification of 2,4-D by plant species, or the concentration of 2,4-D varies with plant species.