二氟乙酸乙酯置于sodium Ethanolate,盐酸,水体系中,用 乙酸乙酯 作为反应溶剂,化学反应 2.0H,以73%的收率获得产物4,4-二氟乙酰乙酸乙酯 参考文献:Novel Imidazole Derivatives Useful For The Treatment Of Arthritis 标题:Novel Imidazole Derivatives Useful For The Treatment Of Arthritis 摘要:本发明提供了以下式的化合物: 其中a,X和r1-R6如本文所述,其药用盐,以及含有该化合物的药物组合物;使用其中一种化合物或其药用盐治疗与骨关节炎相关的疼痛的方法,以及制备这些化合物的方法.
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:CN-108084093-A 优先权日:2017-12-21 标题:One-pot synthesis of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid
专利号:CN-107876092-A 优先权日:2017-11-24 标 题 :High Stability Titanium Catalyst for the Synthesis of Benzyl Carbonate and Diphenyl Carbonate by Transesterification
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
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 131. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 197. 摘要:Chebanov, V. A.; Gorobets, N. Yu.; Sedash, Yu. V., Science of Synthesis: Multicomponent Reactions, (2013) 1, 36.