CAS: 657408-07-6; Dicyclohexyl(2',6'-Dimethoxy-[1,1'-Biphenyl]-2-yl)Phosphine

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CAS号16523-54-9 二环己氯化膦 | CAS号755017-61-9 2'-溴-2,6-二甲氧基-1... | CAS号694-80-4 2-溴氯苯 | CAS号151-10-0 间苯二甲醚 | CAS号23112-96-1 2,6-二甲氧基苯硼酸 | CAS号95-50-1 邻二氯苯 | CAS号27012-22-2 5-甲基-2-苯基吡啶

2-溴氯苯置于正丁基锂体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 5.75H,反应生成 2-双环己基膦-2',6'-二甲氧基联苯
参考文献:铃木-宫浦偶联过程的催化剂:配体结构影响的范围和研究
标题:铃木-宫浦偶联过程的催化剂:配体结构影响的范围和研究
摘要:芳基和杂芳基卤化物与芳基-,杂芳基-和乙烯基硼酸的 Suzuki-Miyaura 偶联反应使用 2-(2',6'-二甲氧基联苯) 二环己基膦 Sphos (1) 以非常好的收率进行.这种配体为这些过程提供了前所未有的活性,允许在低催化剂水平下进行反应,制备极受阻的联芳基化合物,并且通常在室温下进行芳基氯的反应.此外,还介绍了各种 1.Pd 配合物的结构研究以及有助于阐明 1 对 Suzuki-Miyaura 偶联过程的功效的计算数据.此外,与 1 和 2-(2',4',6'-三异丙基联苯)二苯基膦(2)在确定配体体积和给电子能力在源自此类配体的催化剂的高活性中的相对重要性方面提供了信息.此外,当芳基溴变得太受阻时,一个有趣的 Ch 键官能化-交叉偶联序列会介入以提供高产率的产物.
DOI:10.1021/ja042491J

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-10711138-B2
优先权日:2016-04-08
标题:Intermediates and procedures for the synthesis of functional materials
发明人：KIRSCH PEER; GUNST SUSANN
权利人:MERCK PATENT GMBH
摘要:The present invention relates to heteroaromatic compounds which have two different reactive groups, their use in the synthesis of asymmetrically substituted compounds, and synthesis processes in which the compounds according to the invention are reacted sequentially with two different compounds, whereby an asymmetrically substituted compound is formed.

专利号:WO-2025119975-A1
优先权日:2023-12-04
标 题:A method for synthesis of harmine
发明人：HETT ROBERT; GRAB HANUSCH; LAGOUTTE ROMAN
权利人:RECONNECT LABS AG
摘要:The invention relates to a method of synthesis of a compound of formula (I), harmine, according to the method comprising a step of transforming the compound of formula (II), into the compound of formula (I). The invention further relates to a compound of formula (II), which is an intermediate in synthesis of harmine according to the present invention.

专利号:US-12312325-B2
优先权日:2022-03-01
标 题:Methods and compounds useful in the synthesis of an AAK1 inhibitor
发明人：CHEN TAO; WU WENXUE; YAN JUN; ZENG XIANGLU; ZHAO MATTHEW MANGZHU
权利人:LEXICON PHARMACEUTICALS INC
摘要:Methods for the synthesis of (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and salts thereof are disclosed, as well as compounds useful therein.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as