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An Atom-Efficient Route to Ethyl 3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxylate (DFMMP)—A Key Building Block for a Novel Fungicide Family
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2014-07-10 00:00:00 , DOI: 10.1021/op500128p
Janis Jaunzems 1 , Max Braun 1
Affiliation  

A growing number of fluorine-containing active ingredients in the pharmaceutical and agrochemical industries inevitably raises the demand for new fluorinated building blocks. Their availability is mainly constricted by suitable chemistry and available bulk fluorine containing starting materials. Because of the high cost impact especially in the agrochemical industry, the choice of a synthetic route is heavily driven by economic aspects; thus, the environmental profile often is handled as a “secondary factor” or finally falls aside. DFMMP is a key building block for a fast growing new fungicide family, like Syngenta’s Sedaxane, and BASF’s Fluxapyroxad and Bayer’s Bixafen currently made by environmetally less friendly routes. Herein we present a cost-competitive and green route, developed at Solvay laboratories, displaying significantly lower environmental impact.

中文翻译:

原子有效途径生成3-(二氟甲基)-1-甲基-1 H-吡唑-4-羧酸乙酯(DFMMP)-新型杀菌剂家族的关键组成部分

制药和农业化学工业中越来越多的含氟活性成分不可避免地增加了对新型氟化构件的需求。它们的可用性主要受到合适的化学物质和可用的大量含氟起始原料的限制。由于特别是在农用化学工业中的高成本影响,合成路线的选择在很大程度上受到经济方面的驱动。因此,环境状况通常被视为“次要因素”或最终被抛在一边。DFMMP是快速增长的新型杀菌剂家族的重要组成部分,例如先正达公司的Sedaxane,巴斯夫的Fluxapyroxad和拜耳的Bixafen,目前都是通过环境友好的路线生产的。在此,我们介绍了由索尔维实验室开发的具有成本竞争力的绿色路线,
更新日期:2014-07-10
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