二甲基亚砜,溴甲苯,铜 反应 6.0H,以52%的收率获得产物溴化亚铜二甲硫醚 参考文献:Route Optimization And Synthesis Of Taxadienone 标题:Route Optimization And Synthesis Of Taxadienone 摘要:Early Process Development Toward The Scalable Production Of Taxadienone On A Decagram Scale Is Described. A Continuous Flow Reactor Was Employed To Safely Run A Potentially Hazardous Cyclopropane Ring Opening. The Route Featured Two Copper-Mediated Additions,A Diels-Alder Reaction And A Palladium-Catalyzed Negishi Coupling,To Construct The Final Structure. DOI:10.1021/op500314C
专利号:US-2022267266-A1 优先权日:2019-07-09 标 题 :Improved, cost effective process for synthesis of vitamin d3 and its analogue calcifediol from ergosterol 发明人:DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; PRABHU MANOJKUMAR SADANAND; KADAM SACHIN VASANT 权利人:FERMENTA BIOTECH LTD 摘要:Disclosed herein is an improved and efficient process for synthesis of vitamin D3 and its analogue Calcifediol from Ergosterol. Particularly, the present invention discloses the synthesis of key intermediate 3β-tert-Butyldimethylsilyloxy-22-hydroxy-23,24-bisnorchola-5,7-diene (5), and novel intermediate β-tert-Butyldimethylsilyloxy-22-iodo-23,24-bisnorchola-5,7-diene (9) by a simple and cost effective process. The industrially viable processes for preparation of said intermediate(s) results in providing provitamins with various side chains and the desired products in high yield.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:WO-9425396-A3 优先权日:1993-04-27 标题:Process for synthesis of aluminum powder with low oxigen content 发明人:POROWSKI SYLWESTER; JUN JAN; GRZEGORY IZABELLA; BOCKOWSKI MICHAL; WROBLEWSKI MIROSLAW 权利人:CT BADAN WYSOKOCISNIENIOWYCH; POROWSKI SYLWESTER; JUN JAN; GRZEGORY IZABELLA; BOCKOWSKI MICHAL; WROBLEWSKI MIROSLAW 摘要:The method is used for the synthesis of an oxygen less powder of Aluminum Nitride. As an initial material for the reaction a bulk piece of alumina is used (e.g. in the form of a rod or ball) instead of the aluminum powder most frequently used until now. The reaction proceeds in a gas atmosphere with elevated pressure from 10 to 10 000 atm of nitrogen with 5 to 95 % dopes of the nobel gases (e.g. argon, helium) in the temperature region from 200° to 2200 °C. The product of the reaction is a fine powder of Aluminum Nitride.
专利号:US-6603015-B2 优先权日:1999-03-29 标题:Synthesis of epothilones 发明人:GEORG GUNDA I; NAIR SAJIV K; REIFF EMILY; TUNOORI ASHOK RAO 权利人:UNIV KANSAS 摘要:Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
专利号:US-2016317682-A1 优先权日:2015-04-30 标题:PREPARATION OF Ag18F AND ITS USE IN THE SYNTHESIS OF PET RADIOTRACERS 发明人:SCOTT PETER J H; BROOKS ALLEN F; ICHIISHI NAOKO; SANFORD MELANIE S 权利人:UNIV MICHIGAN REGENTS; THE REGENTS OFTHE UNIV OF MICHIGAN 摘要:Copper-catalyzed radiofluorination of aryl iodides using Ag 18 F, methods of preparing Ag 18 F, and compounds obtained by copper-catalyzed radiofluorination of aryl iodides using Ag 18 F are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.
专利号:US-6033624-A 优先权日:1995-02-15 标题 :Methods for the manufacturing of nanostructured metals, metal carbides, and metal alloys 发明人:GONSALVES KENNETH E; RANGARAJAN SRI PRAKASH 权利人:UNIV CONNETICUT 摘要:Methods for the manufacture of nanostructured metals, metal carbides, and metal alloys are presented, such metals including nanostructured aluminum, chromium, iron, molybdenum, vanadium, and steel. Preferably, the nanostructured steel is of the M50 type, and comprises iron, molybdenum, chromium, vanadium and carbon. Synthesis of M50 steel further comprising nanostructured aluminum, aluminum oxide, or aluminum nitride is also described. In accordance with an important feature of this invention, the grain size of the metals and metal alloys is in the nanometer range. In accordance with the method of the present invention, the nanostructured metals, metal carbides, and metal alloys are prepared via chemical synthesis from aluminum, iron, molybdenum, chromium and vanadium starting materials. Decomposition of metal precursors or co-precipitation or precipitation of metal precursors is followed by consolidation of the resulting nanostructured powders. Alternatively, nanostructured M50 steel may be obtained by mixing of nanocrystalline chromium, iron, molybdenum, and vanadium powders, followed by ball-milling, and consolidation. The nanostructured metals, metal carbides, and metal alloys of this invention find particular utility in the manufacture of cutting tools and bearings, and in ferrofluids, magnetic memory systems, and catalysis.
[参考文献]: Beatriz Pacheco Berciano, Et Al. 1,1-Dibromo-1-Alkenes As Valuable Partners In The Copper-Catalyzed Direct Alkynylation Of Azoles. Org Lett. 2010 Sep 17;12(18):4038-41.
合成参考文献
摘要:Aitken, R. A.; Aitken, K., Science of Synthesis, (2008) 43, 606. 摘要:Aitken, R. A.; Aitken, K., Science of Synthesis, (2008) 43, 618. 摘要:Yus, M.; Foubelo, F., Science of Synthesis, (2010) 47, 1107. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 77. 摘要:Cherkinsky, M.; Levinger, S., Science of Synthesis, (2010) 47, 482.