专利号:US-2022372000-A1 优先权日:2021-05-05 标 题:New Process for the Synthesis of 5-Fluoro-3-(Difuoromethyl)-5-Fluoro-1-Methyl-1H-Pyrazole-4-Carboxylic Acid Derivatives and the Free Acid Thereof 发明人:LUO WEIFEN; WU WENTING 权利人:FUJIAN YONGJING TECH CO LTD 摘要:The invention provides a new process for the synthesis of 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid derivatives and the free acid thereof, involving a direct fluorination reaction with a fluorination gas comprising or consisting of elemental fluorine (F2), in a reactor which is resistant to elemental fluorine (F2) and hydrogen fluoride (HF), and wherein in the process as a starting material a difluoromethyl-pyrazole compound dissolved in an inert solvent is subjected to the direct fluorination reaction. Some particular examples of 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid derivatives which can be prepared according to the process of the invention are 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid fluoride (5F-DFMPAF), also known under the alternative name 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carbonyl fluoride; 3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid ethylester (5F-DFMP); and 3-(chlorodifluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid ethylester (5F-CDFMP), or the corresponding methyl esters. The 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid can be obtained from its carboxylic acid derivatives such as, e.g., mentioned before in that the acid derivative is converted to the corresponding carboxylic acid.
专利号:US-9809534-B1 优先权日:2014-07-21 标 题 :Difluoroalkylcyclopropyl amino acids and esters, and syntheses thereof 发明人:LUKIN KIRILL A; MEI JIANZHANG; HILL DAVID R; ABRAHAMSON MICHAEL J 权利人:ABBVIE INC 摘要:The invention provides methods of synthesizing compounds in an asymmetric or enantioenriched fashion, wherein the compounds are useful intermediates in the synthesis of viral protease inhibitors.
专利号:EP-4103553-A1 优先权日:2021-05-05 标 题:New process for the synthesis of 5-fluoro-3- (difuoromethyl) -5-fluoro-1-methyl-1h-pyrazole-4-carboxylic acid derivatives and the free acid thereof
专利号:CN-114450269-A 优先权日:2021-05-05 标题:A new method for the synthesis of 5-fluoro-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxylic acid derivatives and their free acids
专利号:CN-118852012-A 优先权日:2024-09-26 标 题:Synthesis method of high-yield difluoro pyrazole acid
专利号:CN-118515614-A 优先权日:2024-05-21 标 题:Synthesis method of difluoro pyrazole acid
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