羰基硫置于cobalt (III) Fluoride体系中,化学反应生成氟光气 参考文献:Fluorination Of Carbon Disulfide And Carbonyl Sulfide 标题:Fluorination Of Carbon Disulfide And Carbonyl Sulfide 摘要: Doi:10.1021/ja01142A527
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-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
专利号:US-2015336866-A1 优先权日:2013-01-01 标题:Synthesis of difluoromethyl ethers and sulfides 发明人:HARTWIG JOHN; FIER PATRICK 权利人:UNIV CALIFORNIA 摘要:The synthesis of difluoromethyl ethers and sulfides with a simple, non-ozone-depleting reagent is described. The difluoromethylation of phenols with this reagent occurs at room temperature within minutes with exceptional functional group tolerance. The mild conditions makes possible tandem processes for the conversion of aryl boronic acids, aryl halides and arenes to difluoromethyl ethers. Mechanistic studies support a reaction pathway involving nucleophilic attack of the phenolate to difluorocarbene.
专利号:WO-2024010785-A1 优先权日:2022-07-08 标 题:Ketoreductase enzymes for the synthesis of 1,3-diol substituted indanes 发明人:CAHN JACKSON KENAI BLENDER; CHEUNG-LEE WAI LING; CHUN STEPHANIE W; HIRAGA KAORI; KOSJEK BIRGIT; KNIGHT JOHN H; MAKAREWICZ AMANDA M; MCCANN SCOTT; MOORE JEFFREY C; VERMA DEEPTAK 权利人:MERCK SHARP & DOHME LLC 摘要:The present disclosure provides ketoreductase enzymes having improved enzymatic properties including the capability of reducing hydroxy indanones to provide diastereomerically pure 1,3-indane diols useful for the synthesis of belzutifan. Also provided are polynucleotides encoding the ketoreductase enzymes, and host cells capable of expressing the ketoreductase enzymes. A purification procedure for isolating the ketoreductase enzymes is also provided.
专利号:US-4756739-A 优先权日:1985-12-21 标题 :Pyridine derivatives and the N-oxides thereof, and the use thereof as intermediates for the synthesis of plant protecting agents 发明人:FUSS ANDREAS; KOCH VOLKER 权利人:HOECHST AG 摘要:The compounds of the formula I (I) in which A denotes N or N->O, Z denotes O or NH, R denotes H, (halo)alkyl, (halo)alkenyl, (halo)alkynyl or alkoxycarbonyl, R1 denotes hydrogen, halogen, amino, -NHOH, hydroxyl, (substituted) phenylazo or a radical of the formulae Y=C=N-, Y1Y2C=N-, Y3NH- or K denotes 0 or 1, and m and n, independently of one another, denote a number from 1 to 4, with the proviso that, when Z-R denotes OH or NH2, (R1)n denotes at least one radical of the formula or represents two radicals, in the 5 or 6 position of the heterocyclic ring, which, in the 5 position, denote halogen and, in the 6 position, denote a radical of the group comprising halogen, amino, hydroxyl or phenylazo, which may be substituted as specified above, are valuable intermediates in the synthesis of plant protection agents.
专利号:US-5786515-A 优先权日:1995-09-15 标题 :Synthesis of α-chloro or fluoro ketones 发明人:DOLLING ULF H; FREY LISA F; TILLYER RICHARD D; TSCHAEN DAVID M 权利人:MERCK & CO INC 摘要:A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.