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除草剂研究五十年:对比氟乐灵和甲磺草胺的发现。

Fifty years of herbicide research: comparing the discovery of trifluralin and halauxifen-methyl.

机构信息

Dow AgroSciences LLC, Indianapolis, IN, USA.

出版信息

Pest Manag Sci. 2018 Jan;74(1):9-16. doi: 10.1002/ps.4657. Epub 2017 Aug 24.

DOI:10.1002/ps.4657
PMID:28675627
Abstract

Fifty years separate the commercialization of the herbicides trifluralin and halauxifen-methyl. Despite the vast degree of technological change that occurred over that time frame, some aspects of their discovery stories are remarkably similar. For example, both herbicides were prepared very early in the iterative discovery process and both were developed from known lead compound structures by hypothesis-driven research efforts without the use of in vitro assays or computer-aided molecular design. However, there are aspects of the halauxifen-methyl and trifluralin discovery stories that are substantially different. For example, the chemical technology required for the cost-effective production of halauxifen-methyl simply did not exist just two decades prior to its commercial launch. By contrast, the chemical technology required for the cost-effective production of trifluralin was reported in the chemical literature more than two decades prior to its commercial launch. In addition, changes in regulatory environment since the early 1960s ensured that their respective discovery to commercial launch stories would also differ in substantial ways. Ultimately, the time and cost required to develop and register halauxifen-methyl demanded a global initial business case while the lower registration hurdles that trifluralin cleared enabled a narrow initial business case mainly focused on the USA. © 2017 Society of Chemical Industry.

摘要

五十年前,两种除草剂氟乐灵和halauxifen-甲基实现了商业化。尽管在这段时间里发生了巨大的技术变革,但它们的发现故事仍有一些惊人的相似之处。例如,这两种除草剂都是在迭代发现过程的早期制备的,并且都是通过假设驱动的研究工作从已知的先导化合物结构中开发出来的,没有使用体外测定或计算机辅助分子设计。然而,halauxifen-甲基和氟乐灵的发现故事在某些方面有很大的不同。例如,在其商业化推出仅仅二十年前,用于生产 halauxifen-甲基的经济有效的化学技术根本不存在。相比之下,在其商业化推出二十多年前,氟乐灵的经济有效的生产所需的化学技术就在化学文献中有报道。此外,自 20 世纪 60 年代初以来监管环境的变化确保了它们各自的发现到商业化推出的故事也会有很大的不同。最终,开发和注册 halauxifen-甲基所需的时间和成本要求一个全球性的初始商业案例,而氟乐灵清除的较低注册障碍使一个主要集中在美国的狭窄初始商业案例成为可能。 © 2017 化学工业协会。

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