邻二氯苯置于sodium体系中,用 N,N-二甲基乙酰胺 用作溶剂,化学反应 39.0H,反应生成1,2-苯二硫醇 参考文献:Simple Syntheses Of Aryl Alkyl Thioethers And Of Aromatic Thiols From Unactivated Aryl Halides And Efficient Methods For Selective Dealkylation Of Aryl Alkyl Ethers And Thioethers 标题:Simple Syntheses Of Aryl Alkyl Thioethers And Of Aromatic Thiols From Unactivated Aryl Halides And Efficient Methods For Selective Dealkylation Of Aryl Alkyl Ethers And Thioethers 摘要: Doi:10.1055/s-1983-30501
专利号:WO-2024189634-A1 优先权日:2023-03-13 标 题 :Highly atom economical process for synthesis of novel co-initiator for photo-induced radical polymerisation 发明人:KAPAT DR AJOY; AHMAD ASRAR; MITTAL GARVISHA 权利人:SHIV NADAR INSTITUTION OF EMINENCE DEEMED TO BE UNIV 摘要:The present invention relates to a base catalyzed sequential conjugate addition reaction for the synthesis of a novel and efficient co-initiator for Photo Induced Radical Polymerization. The process comprises synthesis of new co-initiator having 6,5 and 6,6-bicyclic scaffolds as central core. The process comprises reacting thiocarboxylic acid, catechol, thiocatechol, benzodithiol, benzothiocatechol and binol with ketone substrates at room temperature with a base and a solvent to yield the novel co-initiator compound of Formula 3, Formula 5, Formula C and Formula Z.
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:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 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 a wide variety of substituents at position 5 of the tetracycline ring system.
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:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
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合成参考文献
参考文献:10.1007/s10337-010-1878-1 摘要:Wilson EA, Ennahar S, Zhao M, Bergaentzle M, Marchioni E, Bindler F. Simultaneous Determination of Various Isothiocyanates by RP-LC Following Precolumn Derivatization with Mercaptoethanol. Chromatographia. 2011 Jan 08;73(Suppl 1):137–42. doi: 10.1007/s10337-010-1878-1.