2-硝基碘苯置于盐酸,苯基氯化镁体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 0.58H,反应生成 2-硝基苯基硼酸 参考文献:Promoting Reductive Tandem Reactions Of Nitrostyrenes With Mo(Co)6 And A Palladium Catalyst To Produce 3H-Indoles 标题:Promoting Reductive Tandem Reactions Of Nitrostyrenes With Mo(Co)6 And A Palladium Catalyst To Produce 3H-Indoles 摘要:The Combination Of Mo(Co)(6) And 10 Mol % Of Palladium Acetate Catalyzes The Transformation Of 2-Nitroarenes To 3H-Indoles Through A Tandem Cyclization-[1,2] Shift Reaction Of In Situ Generated Nitrosoarenes. Mo(Co)(6) Appears To Have Dual Roles In This Transformation Generate Generate Co And Promote C-N Bond Formation To Increase The Yield Of The N-Heterocycle Product. DOI:10.1021/jacs.5B02946
专利信息
专利号:US-11738092-B2 优先权日:2019-12-04 标题:Methods and compositions for synthesis of therapeutic nanoparticles 发明人:WYENT EMILY A; BLUMENFELD CARL M; LAMM ROBERT J 权利人:DANTARI INC 摘要:Improved methods and reactants for the chemical synthesis of therapeutic nanoparticles are provided. The nanoparticles comprise a polymeric core, to which is attached one or more homing molecules and one or more therapeutic agents. Improvements in speed, yield and purity are attained using the methods disclosed herein.
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:US-7902196-B2 优先权日:2005-03-17 标 题 :Synthesis of avrainvillamide, strephacidin B, and analogues thereof 发明人:MYERS ANDREW G; HERZON SETH B; WULFF JEREMY EARLE; SIEGRIST ROMAIN; SVENDA JAKUB; ZAJAC MATTHEW ALLEN 权利人:HARVARD COLLEGE 摘要:The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection.
专利号:US-5254776-A 优先权日:1992-07-17 标 题:Synthesis of bromobiphenyls 发明人:LANG JOHN F; GURUSAMY NARAYANASAMY 权利人:MALLINCKRODT SPEC CHEM 摘要:Bromobiphenyls (such as 2-fluoro-4-bromobiphenyl) are synthesized by reacting together a phenylboronic acid (such as phenylboronic acid) and a bromoiodobenzene (such as 2-fluoro-4-bromoiodobenzene). The reaction generally takes place with the aid of a catalyst (such as palladium in a zero valance state) and an inert solvent (such as fluorobenzene). Control of temperature is very important to obtain both an acceptable reaction rate and an acceptable level of terphenyl byproduct.
专利号:US-2023355800-A1 优先权日:2019-12-04 标 题 :Methods and compositions for synthesis of therapeutic nanoparticles
专利号:WO-02057274-A1 优先权日:2001-01-19 标题 :A process for the synthesis of atorvastatin form v and phenylboronates as intermediate compounds
[参考文献]: Raquel Rodríguez González, Et Al. Synthesis Of 2-Nitro- And 2,2'-Dinitrobiphenyls By Means Of The Suzuki Cross-Coupling Reaction. J Org Chem. 2005 Nov 11;70(23):9591-4.
合成参考文献
摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 268. 摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 73. 参考文献:10.1016/j.jchromb.2006.07.060 摘要:Rozet E, Morello R, Lecomte F, Martin GB, Chiap P, Crommen J, Boos KS, Hubert P. Performances of a multidimensional on-line SPE-LC-ECD method for the determination of three major catecholamines in native human urine: validation, risk and uncertainty assessments. J Chromatogr B Analyt Technol Biomed Life Sci. 2006 Dec 05;844(2):251–60. doi: 10.1016/j.jchromb.2006.07.060.