2-Phenoxyphenyl Pivalate置于bis(1,5-Cyclooctadiene)Nickel (0),Caesium Carbonate,1,2-双(二环己基磷基)-乙烷体系中,用 5,5-Dimethyl-1,3-Cyclohexadiene 用作溶剂,化学反应 72.0H,以66%的收率获得二苯并呋喃 参考文献:Nickel-Catalyzed Intramolecular C-h Arylation Using Aryl Pivalates As Electrophiles 标题:Nickel-Catalyzed Intramolecular C-h Arylation Using Aryl Pivalates As Electrophiles 摘要:This Paper Describes A Method For Nickel Catalyzed Intramolecular C-H Arylation Using Aryl Pivalates As Electrophiles. The Transformation Is Efficient For The Synthesis Of Diverse Electronically And Sterically Differentiated Dibenzofurans. Additionally,The Method Could Be Expanded Toward The Synthesis Of Carbazoles. Preliminary Mechanistic Studies Of The Transformation Are Also Described. (C) 2013 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tet.2013.04.096
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
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-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:US-8569560-B2 优先权日:2006-10-13 标题 :Synthesis of terminal alkenes from internal alkenes via olefin metathesis 发明人:SCHRODI YANN; PEDERSON RICHARD L; KAIDO HIROKI; TUPY MICHAEL J 权利人:ELEVANCE RENEWABLE SCIENCES 摘要:This disclosure relates generally to olefin metathesis, and more particularly relates to the synthesis of terminal alkenes from internal alkenes using a cross-metathesis reaction catalyzed by an olefin metathesis catalyst. According to one aspect, for example, a method is provided for synthesizing a terminal olefin, the method comprising contacting, in the presence of a ruthenium alkylidene metathesis catalyst, an olefinic substrate comprised of at least one internal olefin with a cross metathesis partner comprised of an alpha olefinic reactant, under reaction conditions effective to allow cross-metathesis to occur, wherein the reaction conditions include a reaction temperature of at least 35° C. The methods, compositions, reactions and reaction systems herein disclosed have utility in the fields of catalysis, organic synthesis, and industrial chemistry.
专利号:US-2017327504-A1 优先权日:2014-10-30 标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines 发明人:ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD 权利人:SANDOZ AG 摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.
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.
1: Bhagwat AA, Mohbiya DR, Avhad KC, Sekar N. Viscosity-active D-π-A chromophores derived from benzo[b]thiophen-3(2H)-one 1,1-dioxide (BTD): Synthesis, photophysical, and NLO properties. Spectrochim Acta A Mol Biomol Spectrosc. 2018 May 29;203:244-257. doi: 10.1016/j.saa.2018.05.101. [Epub ahead of print] doi: 10.1016/j.scitotenv.2018.05.257. [Epub ahead of print] doi: 10.1021/acs.joc.8b00792. Epub 2018 May 24. doi: 10.1080/13543776.2018.1472239. Epub 2018 May 9. Review. doi: 10.1016/j.jhazmat.2018.04.057. Epub 2018 Apr 25. doi: 10.1021/acs.est.8b01028. Epub 2018 May 2. doi: 10.1039/c8em00033f. doi: 10.3389/fphar.2018.00265. eCollection 2018. 10: Peng A, Gao J, Chen Z, Wang Y, Li H, Ma LQ, Gu C. Interactions of Gaseous 2-Chlorophenol with Fe(3+)-Saturated Montmorillonite and Their Toxicity to Human Lung Cells. Environ Sci Technol. 2018 May 1;52(9):5208-5217. doi: 10.1021/acs.est.7b06664. Epub 2018 Apr 10. doi: 10.1021/acs.est.7b04633. Epub 2018 Apr 11. doi: 10.1016/j.bmcl.2018.03.048. Epub 2018 Mar 19. doi: 10.1016/j.wasman.2018.03.006. Epub 2018 Mar 21. pii: E23. doi: 10.3390/ph11010023. 15: Takahashi S, Kawano T, Nakajima N, Suda Y, Usukhbayar N, Kimura KI, Koshino H. Synthesis of polyozellin, a prolyl oligopeptidase inhibitor, and its structural revision. Bioorg Med Chem Lett. 2018 Mar 1;28(5):930-933. doi: 10.1016/j.bmcl.2018.01.054. Epub 2018 Jan 31. doi: 10.1098/rsos.171079. eCollection 2018 Jan.
合成参考文献
参考文献:10.1021/es902648t 摘要:Truong H, Lomnicki S, Dellinger B. Potential for misidentification of environmentally persistent free radicals as molecular pollutants in particulate matter. Environ Sci Technol. 2010 Mar 15;44(6):1933–9. 参考文献:10.1021/jo1000803 摘要:Benniston AC, Copley G, Harriman A, Howgego D, Harrington RW, Clegg W. Cofacial boron dipyrromethene (Bodipy) dimers: synthesis, charge delocalization, and exciton coupling. J Org Chem. 2010 Mar 19;75(6):2018–27. doi: 10.1021/jo1000803. 参考文献:10.1016/j.chemosphere.2011.06.035 摘要:Aristizábal BH, Gonzalez CM, Morales L, Abalos M, Abad E. Polychlorinated dibenzo-p-dioxin and dibenzofuran in urban air of an Andean city. Chemosphere. 2011 Sep;85(2):170–8. doi: 10.1016/j.chemosphere.2011.06.035. 参考文献:10.1007/s11356-011-0561-x 摘要:Turgut C, Atatanir L, Mazmanci B, Mazmanci MA, Henkelmann B, Schramm K. The occurrence and environmental effect of persistent organic pollutants (POPs) in Taurus Mountains soils. Environmental Science and Pollution Research. 2011 Jul 13;19(2):325–34. doi: 10.1007/s11356-011-0561-x. 参考文献:10.1021/jm200004e 摘要:Gokhale A, Weldeghiorghis TK, Taneja V, Satyanarayanajois SD. Conformationally constrained peptides from CD2 to modulate protein-protein interactions between CD2 and CD58. J Med Chem. 2011 Aug 11;54(15):5307–19.