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:WO-2017089470-A1 优先权日:2015-11-27 标 题:Process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases 发明人:HOFMANN DAGMAR; HOFMANN JOSEFA; HEINRICH MARKUS 权利人:Friedrich-Alexander-Universität Erlangen-Nürnberg 摘要:The present invention relates to a process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases.
专利号:US-2013338369-A1 优先权日:2011-03-07 标 题 :Process for the Synthesis of Aminobiphenylene 发明人:HEINRICH MARKUS; PRATSCH GERALD 权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE 摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
专利号:US-8629288-B2 优先权日:2008-02-25 标题:Method for the regioselective synthesis of 1-alky1-3-haloalkyl-pyrazole-4-carboxylic acid derivatives 发明人:PAZENOK SERGII; LUI NORBERT; HEINRICH JENS-DIETMAR; WOLLNER THOMAS 权利人:PAZENOK SERGII; LUI NORBERT; HEINRICH JENS-DIETMAR; WOLLNER THOMAS; BAYER IP GMBH 摘要:The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives, and to the hydrazones formed as intermediates in the process.
专利号:WO-2021033172-A1 优先权日:2019-08-20 标题:Process for the preparation of chlorantraniliprole 发明人:V ASHWIN; PRADHAN ASHOK KUMAR; PALIMKAR SANJAY SAMBHAJIRAO; MANE AVINASH SHESHRAO; KUNHIMON SYAM KUMAR UNNIARAN 权利人:EUROFINS ADVINUS LTD 摘要:The present invention relates to two novel, efficient and one-pot methods for synthesizing chlorantraniliprole. In the first scheme, Chlorantraniliprole is prepared by a novel telescopic process starting from 3-Bromo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxylic acid a key raw material-A (Key RM-A). In the second scheme, starting from Key RM-A, the process steps use of a novel variant of anthranilic acid (Methyl 2-amino-5-chloro-3-methylbenzoate), to get Chlorantraniliprole. Furthermore, the present invention also relates to the synthesis of key starting material for the synthesizing chlorantraniliprole in-situ. All the in-situ steps of the disclosed synthesis methods obtain good yield, without using any expensive reagent or base or harsh reaction conditions, which makes the process simple, environment friendly and more cost effective. With this process the production cost of chlorantraniliprole and its intermediates is substantially reduced; fewer by-products are formed during its synthesis and since it's a one-pot reaction, isolation and purification are easy to achieve.
专利号:US-2006069270-A1 优先权日:2004-09-27 标 题 :Process for the preparation of 1,3,5-trisubstituted pyrazoles via [3+2] cycloaddition 发明人:SHAPIRO RAFAEL; ROSSANO LUCIUS T; TENHUISEN KAREN L 权利人:SHAPIRO RAFAEL; ROSSANO LUCIUS T; TENHUISEN KAREN L 摘要:A process for the preparation of 1,3,5-trisubstituted pyrazole compounds, which are useful intermediates in the synthesis of factor Xa inhibitors.