1,4-二氟苯置于potassium Permanganate体系中,化学反应生成2,5-二氟苯甲酸 参考文献:Fragmentation Of Radical Anions Of Polyfluorinated Benzoates 标题:Fragmentation Of Radical Anions Of Polyfluorinated Benzoates 摘要:A Comprehensive Study Of The Symmetry Forbidden Fragmentation Of Short-Lived Radical Anions (Ras) Has Been Undertaken For The Complete Set Of Polyfluorinated Benzoates (C6Fnh5-Nco2-,N = 1-5) The Decay Rate Constants (K(C)) Of Ras Have Been Determined In Aqueous Alkaline Solution (Ph 13.4) By Electron Photoinjection (Epi) From Mercury Electrodes And Were Found To Increase Dramatically From Less Than Or Equal To 3 X 10(3) S(-1) (3-F-C6H4Co2-) To (1.2 +/-0.8) X 10(9) S(-1) (C6F5Co2-). The Regioselectivity Of C-F Bond Cleavage In The Ra Fragmentation Has Been Revealed By Structure Assignment Of Reduction Products Of The Polyfluorinated Benzoic Acids By Na,K,And Zn In Liquid Nh3,As Well As By Zn In Aqueous Nh3 And Aqueous Alkaline Solutions. The K(C) Values Depend On The Position Of The Cleaved Fluorine To The Co2-Group Generally In The Order Para > Ortho > Meta,And To Sharply Increase If Adjacent Fluorine Atoms Are Present. The Observed Trends Reveal That The Kinetics Of The Ra Fragmentation Reaction Is Not Controlled By The Reaction Thermodynamics. Semiempirical Uhf/indo Calculations,The Validity Of Which Has Been Confirmed By Ab Initio Rohf/6-31+g Calculations,Were Done To Rationalize The Observed Trends. The Reaction Transition State (Ts) Was Considered To Arise From The Ra'S Ii And Sigma* States Crossing Avoided Due To Out-Of-Plane Deviation Of The Cleaving C-F Bond. The Satisfactory Linear Correlation (R = 0.96) Between The Model Reaction Energy Barrier E-A And Log K(C) Has Been Achieved With Modeling The Local Solvation Of The Co2-Group By Its Protonation. Doi:10.1021/jp993361D
专利号:US-11999757-B2 优先权日:2017-11-01 标 题:Synthesis of boronate ester derivatives and uses thereof 发明人:BOYER SERGE HENRI; HECKER SCOTT J; VERZIJL GERARDUS K M; HERMSEN PETRUS J 权利人:MELINTA SUBSIDIARY CORP 摘要:Disclosed herein are methods for the preparation of boronate derivatives in the synthesis of antimicrobial compounds and uses thereof. Disclosed herein includes method of making a compound of Formula (B) by reducing the ketone group of the keto-ester compound of Formula (A), and the reduction can be performed using a Ruthenium based catalyst system or using an alcohol dehydrogenase bioreduction system.
专利号:US-10669292-B2 优先权日:2014-05-05 标 题 :Synthesis of boronate salts and uses thereof 发明人:HECKER SCOTT; BOYER SERGE 权利人:REMPEX PHARMACEUTICALS INC 摘要:Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-9428524-B2 优先权日:2010-05-25 标 题:Synthetic process for the manufacture of ecteinascidin compounds 发明人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN 权利人:MARTIN LÓPEZ MA JESÚS; FRANCESCH SOLLOSO ANDRÉS; CUEVAS MARCHANTE MARIA DEL CARMEN; PHARMA MAR SA 摘要:This invention relates to compounds of formula II: wherein R 1 , R 2 , Prot SH , and Prot NH are as defined, to processes for the synthesis of ecteinascidins of formula I from compounds of formula II, and to processes for the synthesis of compounds of formula II.
专利号:US-6180830-B1 优先权日:1995-11-08 标题 :Method for preparing a bimetallic ruthenium/tin catalyst and a process for the synthesis of aldehydes 发明人:JACQUOT ROLAND 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a new process for the preparation of a bimetallic ruthenium/tin catalyst. The process for the preparation of a bimetallic ruthenium/tin catalyst according to the invention is characterised by the fact that it consists in carrying out the reduction of a ruthenium complex having an electrovalency of -4 and a coordination number of 6, the ligands being either a halogen atom or an anion or a tin halide. The catalyst is further employed for the preparation of aldehydes by reduction, in the vapor phase, of carboxylic acids, esters and anhydrides.
专利号:US-8487094-B2 优先权日:2008-07-25 标题 :Synthesis of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 发明人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA 权利人:FANDRICK KEITH R; GAO JOE JU; LI WENJIE; LU ZHI-HUI; ZHANG YONGDA; BOEHRINGER INGELHEIM INT 摘要:Disclosed are syntheses of 11β-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
[参考文献]: René K Juhler, Et Al. Analysing Fluorobenzoate Tracers In Groundwater Samples Using Liquid Chromatography-Tandem Mass Spectrometry. A Tool For Leaching Studies And Hydrology. J Chromatogr A. 2002 May 24;957(1):11-6.
合成参考文献
参考文献:10.1007/s00044-016-1756-y 摘要:Popiołek Ł. Hydrazide–hydrazones as potential antimicrobial agents: overview of the literature since 2010. Medicinal Chemistry Research. 2016 Nov 25;26(2):287–301. doi: 10.1007/s00044-016-1756-y.