CAS: 5720-05-8; 4-Tolylboronic Acid

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CAS号106-38-7 对溴甲苯 | CAS号624-31-7 对碘甲苯 | CAS号29540-83-8 三氟甲烷磺酸对甲苯酯 | CAS号121-43-7 硼酸三甲酯 | CAS号106-43-4 对氯甲苯 | CAS号40881-45-6 Dimethyl (4-met... | CAS号195062-57-8 4,4,5,5-四甲基-2-(... | CAS号5419-55-6 硼酸三异丙酯 | CAS号7439-95-4 镁标准溶液 | CAS号688-74-4 硼酸三丁酯 | CAS号10551-32-3 2,5-DIHYDROXY-4... | CAS号108695-61-0 1-methyl-4-(1-n... | CAS号503536-74-1 5-(4-甲基苯基)-2-氨基吡啶 | CAS号36192-63-9 2-氨基-4‘-甲基苯甲酮 | CAS号1204-43-9 4-甲基-联苯-2-胺 | CAS号50670-51-4 4-(4-溴甲基苯基)苯甲腈 | CAS号50670-50-3 4’-氰基-4-甲基联苯 | CAS号3333-13-9 1-烯丙基-4-甲基苯 | CAS号49742-56-5 4’-甲基[1,1’-联苯]-... | CAS号4385-75-5 4-吡啶-3-基苯甲酸

对苄基三氟甲磺酸置于tris(Dibenzylideneacetone)Dipalladium(0) Chloroform Complex,Diisopropopylaminoborane,三乙胺,三苯基膦,甲醇体系中,用 四氢呋喃 作为反应溶剂,化学反应 12.0H,以86%的收率获得产物4-甲苯硼酸
参考文献:Lithium Aminoborohydrides 17. Palladium Catalyzed Borylation Of Aryl Iodides,Bromides,And Triflates With Diisopropylaminoborane Prepared From Lithium Diisopropylaminoborohydride
标题:Lithium Aminoborohydrides 17. Palladium Catalyzed Borylation Of Aryl Iodides,Bromides,And Triflates With Diisopropylaminoborane Prepared From Lithium Diisopropylaminoborohydride
摘要:The Alcaraz-Vaultier Borylation Of Aryl Halides And Triflates Is Reported Utilizing Diisopropylaminoborane (Bh2N(Pr-I)(2)) Prepared From The Corresponding Lithium Aminoborohydride (Lab Reagent). Bh2N(Pr-I)(2) Prepared By Reacting Lithium Diisopropylaminoborohydride With Trimethylsilyl Chloride,Provided The Most Consistent Isolated Yields From This Reaction. Catalytic Amounts Of Palladium Dichloride Produced The Highest Yields From Aryl Iodides,While Catalytic Tris(Dibenzylideneacetone)Dipalladium(Chloroform) Provided The Best Yields For Aryl Bromides And Triflates. This Route To Boronic Acids Is Mild Enough To Tolerate Various Functionalities And For The First Time Employs Aryl Triflates As Substrates For The Alcaraz-Vaultier Borylation. In Addition,It Was Found That Both Boronic Acid And Ester Compounds Could Be Isolated From The Reaction Mixture Utilizing Simple Work-Up Procedures. Treatment Of The Reaction Intermediate With An Acid/base Work-Up Provided The Corresponding Boronic Acid,While Treating The Same Intermediate With A Diol,Such As Neopentyl Glycol,Afforded The Corresponding Boronic Ester. (C) 2010 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Tet.2010.11.065

专利信息

专利号:US-9388131-B2
优先权日:2011-04-27
标题:Automated synthesis of small molecules using chiral, non-racemic boronates
发明人：BURKE MARTIN D; LI JUNQI; GILLIS ERIC P
权利人:UNIV ILLINOIS
摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

专利号:US-9862733-B2
优先权日:2010-07-23
标题 :Apparatus and methods for the automated synthesis of small molecules
发明人：BURKE MARTIN D; GILLIS ERIC P; BALLMER STEVEN G
权利人:BURKE MARTIN D; GILLIS ERIC P; BALLMER STEVEN G; UNIV ILLINOIS
摘要:Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention. Coupling and other reactions embraced by the invention include, without limitation, Suzuki-Miyaura coupling, oxidation, Swern oxidation, “Jones reagents†oxidation, reduction, Evans' aldol reaction, HWE olefination, Takai olefination, alcohol silylation, desilylation, p-methoxybenzylation, iodination, Negishi cross-coupling, Heck coupling, Miyaura borylation, Stille coupling, and Sonogashira copling.

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-6867306-B2
优先权日:2001-01-19
标题:Process for the synthesis of atorvastatin form v and phenylboronates as intermediate compounds
发明人：SRINATH SUMITRA; MATHEW JOY; UJIRE SANDHYA; SRIDHARAN MADHAVAN; SAMBASIVAM GANESH
权利人:BIOCON LTD
摘要:The present invention discusses a novel process for the synthesis of [R-(R*,R*)]-2-(4-fluorophenyl)-B,D-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium, atorvastatin. The compound so prepared is useful as inhibitor of the HMG-CoA reductase and may thus be used as hypolipidemic and hypocholesterolemic agent.

专利号:US-7250510-B2
优先权日:2005-08-24
标 题:Transition metal complexes of N-heterocyclic carbenes, method of preparation and use in transition metal catalyzed organic transformations
发明人：ORGAN MICHAEL G; O'BRIEN CHRISTOPHER J; KANTCHEV ASSAM ERIC B
权利人:TOTAL SYNTHESIS LTD
摘要:The present invention relates to catalysts of transition metal complexes of N-heterocyclic carbenes, their methods of preparation and their use in chemical synthesis. The synthesis, ease-of-use, and activity of the compounds of the present invention are substantial improvements over in situ catalyst generation. Further, the transition metal complexes of N-heterocyclic carbenes of the present invention may be used as precatalysts in metal-catalyzed cross-coupling reactions.