98-80-6 + 586-76-5 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Palladium Solvents: Water; 24 H,27 °C1.2 Reagents: Hydrochloric Acid Solvents: Water 标题:Gold/palladium Alloy For Carbon-Halogen Bond Activation: An Unprecedented Halide Dependence 作者:Dhital,Raghu Nath; Bobuatong,Karan; Ehara,Masahiro; Sakurai,Hidehiro 参考文献:Chemistry - An Asian Journal 日期:2015 卷标:10(12) 页码:2669-2676]
98-80-6 + 586-76-5 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Palladium Solvents: Ethanol,Water; 1 H,60 °C 标题:Ligand-Free,Recyclable Palladium-Functionalized Magnetite Nanoparticles As A Catalyst In The Suzuki-,Sonogashira,And Stille Reaction 作者:De Cattelle,Amaury; Billen,Arne; O'Rourke,Galahad; Brullot,Ward; Verbiest,Thierry; Et Al 参考文献:Journal Of Organometallic Chemistry 日期:2019 卷标:904]
3597-91-9 = 92-92-2 反应条件:1.1 Reagents: Oxygen Catalysts: Manganese Carbonate,Zinc Oxide (Zno),Graphene (Oxide,Reduced) Solvents: Toluene; 11 Min,100 °C 标题:Mixed Zinc/manganese On Highly Reduced Graphene Oxide: A Highly Active Nanocomposite Catalyst For Aerial Oxidation Of Benzylic Alcohols 作者:Assal,Mohamed E.; Shaik,Mohammed Rafi; Kuniyil,Mufsir; Khan,Mujeeb; Alzahrani,Abdulrahman Yahya; Et Al 参考文献:Catalysts 日期:2017 卷标:7(12)]
98-80-6 + 619-58-9 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate Solvents: Water; 0.25 H,80 °C 标题:Catalytic Polymeric Nanocomposites Via Cucurbit[n]Uril Host-Guest Interactions 作者:Wu,Yuchao; Lan,Yang; Liu,Ji; Scherman,Oren A. 参考文献:Nanoscale 日期:2015 卷标:7(32) 页码:13416-13419]
98-80-6 + 586-76-5 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate Catalysts: 1604839-72-6 (Silica-Coated Iron Oxide-Bound) Solvents: Water; 6 H,Rt -> 60 °C 标题:A Highly Water-Dispersible/magnetically Separable Palladium Catalyst Based On A Fe3O4@sio2 Anchored Teg-Imidazolium Ionic Liquid For The Suzuki-Miyaura Coupling Reaction In Water 作者:Karimi,Babak; Mansouri,Fariborz; Vali,Hojatollah 参考文献:Green Chemistry 日期:2014 卷标:16(5) 页码:2587-2596]
98-80-6 + 586-76-5 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate,Oxygen Catalysts: 1590342-82-7 Solvents: Dimethylformamide,Water; 24 H,100 - 110 °C 标题:Efficient Catalysis Of Suzuki-Miyaura Cc Coupling Reactions With Palladium(Ii) Complexes Of Partially Hydrolyzed Bisimine Ligands: A Process Important In Environment Context 作者:Kumar,Arun; Rao,Gyandshwar Kumar; Saleem,Fariha; Kumar,Rupesh; Singh,Ajai K. 参考文献:Journal Of Hazardous Materials 日期:2014 卷标:269 页码:9-17]
98-80-6 + 586-76-5 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate Catalysts: Palladium Solvents: Water; 4 H,100 °C 标题:Palladium(Ii)-(E,N,E) Pincer Ligand (E = S/se/te) Complex Catalyzed Suzuki Coupling Reactions In Water Via In Situ Generated Palladium Quantum Dots 作者:Kumar,Satyendra; Rao,Gyandshwar K.; Kumar,Arun; Singh,Mahabir P.; Singh,Ajai Kumar 参考文献:Dalton Transactions 日期:2013 卷标:42(48) 页码:16939-16948]
720-75-2 = 92-92-2 反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Tetrahydrofuran,Water; 12 H,Rt1.2 Reagents: Sodium Bisulfate; Ph 1,Rt 标题:Preparation Of Pyrrolidinyl Carboxamides As Fatty Acid Synthase Inhibitors For Treating Cancer 参考文献:World Intellectual Property Organization]
14047-29-1 = 92-92-2 反应条件:1.1 Reagents: Potassium Carbonate Catalysts: (Sp-4-2)-[1,1′-Bis[bis(1,1-Dimethylethyl)Phosphino-Kp]Ferrocene]Dichloropalladiu... Solvents: Acetonitrile,Water; 1 - 2 H,60 °C 标题:A Mild Robust Generic Protocol For The Suzuki Reaction Using An Air Stable Catalyst 作者:Moseley,Jonathan D.; Murray,Paul M.; Turp,Edward R.; Tyler,Simon N. G.; Burn,Ross T. 参考文献:Tetrahedron 日期:2012 卷标:68(30) 页码:6010-6017]
98-80-6 + 586-76-5 = 92-92-2 反应条件:1.1 Reagents: Trisodium Phosphate Catalysts: Palladium,Diaion Hp 20 Solvents: Water; 6 H,Rt 标题:Carbon-Carbon Bond Formation By Ligand-Free Cross-Coupling Reaction Using Palladium Catalyst Supported On Synthetic Adsorbent 作者:Monguchi,Yasunari; Sakai,Keita; Endo,Koichi; Fujita,Yuki; Niimura,Masaru; Et Al 参考文献:Chemcatchem 日期:2012 卷标:4(4) 页码:546-558]
3315-91-1 = 92-92-2 反应条件:1.1 Solvents: Tetrahydrofuran; 42 S,4 Atm,Rt1.2 Reagents: Ammonium Hydroxide; Rt1.3 Reagents: Formic Acid Solvents: Tetrahydrofuran 标题:The Continuous-Flow Synthesis Of Carboxylic Acids Using Co2 In A Tube-In-Tube Gas Permeable Membrane Reactor 作者:Polyzos,Anastasios; O'Brien,Matthew; Petersen,Trine P.; Baxendale,Ian R.; Ley,Steven V. 参考文献:Angewandte Chemie 日期:2011 卷标:50(5) 页码:1190-1193]
619-58-9 + 1124-19-2 = 92-92-2 反应条件:1.1 Reagents: Potassium Hydroxide Solvents: Water; Rt1.2 Reagents: Oxygen Catalysts: Palladium; 24 H,Rt1.3 Reagents: Hydrochloric Acid Solvents: Water; Rt 标题:Effects Of The Material Structure On The Catalytic Activity Of Peptide-Templated Pd Nanomaterials 作者:Bhandari,Rohit; Knecht,Marc R. 参考文献:Acs Catalysis 日期:2011 卷标:1(2) 页码:89-98
1-([1,1'-Biphenyl]-4-yl)-2-Tosylethan-1-One置于ammonium Cerium (Iv) Nitrate,氧气体系中,用 乙腈 作为反应溶剂,化学反应 4.0H,以90%的收率获得产物4-苯基苯甲酸 参考文献:Oxidative Cleavage Of α-Sulfonyl Ketones To Carboxylic Acids With Ce(Nh4)2(No3)6 标题:Oxidative Cleavage Of α-Sulfonyl Ketones To Carboxylic Acids With Ce(Nh4)2(No3)6 摘要:Tandem Oxidative Cleavage Of Alpha-Sulfonyl Arylketones 2 With The Combination Of Ce(Nh4)(2)(No3)(6) And O-2 In Mecn Afforded Carboxylic Acids 3 In Moderate To Good Yields. The Plausible Reaction Mechanism Has Been Discussed. (C) 2014 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetlet.2014.08.038
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-11220513-B2 优先权日:2015-04-30 标题:Chromium-mediated coupling and application to the synthesis of halichondrins 发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO 权利人:HARVARD COLLEGE 摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
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.
[参考文献]: Arxel De León, Et Al. Synthesis Of Mercaptopropyl-(Phenylene)S-Benzoates Passivated Gold Nanoparticles: Implications For Plasmonic Photovoltaic Cells. J Colloid Interface Sci. 2015 Oct 15:456:182-9. [参考文献]: H Lygre, Et Al. Biologic Testing Of Leachable Aromatic Compounds From Denture Base Materials. Acta Odontol Scand. 1995 Dec;53(6):397-401. [参考文献]: H Lygre, Et Al. Leaching Of Additives And Degradation Products From Cold-Cured Orthodontic Resins. Acta Odontol Scand. 1994 Jun;52(3):150-6. [参考文献]: H Lygre, Et Al. Leaching Of Organic Additives From Dentures In Vivo. Acta Odontol Scand. 1993 Feb;51(1):45-51. [参考文献]: Loretta Aureli, Et Al. Predicting Human Serum Albumin Affinity Of Interleukin-8 (Cxcl8) Inhibitors By 3D-Qspr Approach. J Med Chem. 2005 Apr 7;48(7):2469-79.
合成参考文献
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 555. 摘要:Ramón, D. J.; Yus, M., Science of Synthesis, (2009) 46, 543. 摘要:Braverman, S.; Cherkinsky, M., Science of Synthesis Knowledge Updates, (2014) 3, 246. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 410. 摘要:Suginome, M.; Ohmura, T., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 171.