📜肉桂醛肟置于bis[dichloro(Pentamethylcyclopentadienyl)Iridium(III)]体系中,用 甲苯 用作溶剂,化学反应 4.0H,以90%的收率获得反-肉桂酰胺 参考文献:Iridium-Catalyzed Conversion Of Alcohols Into Amides Via Oximes 标题:Iridium-Catalyzed Conversion Of Alcohols Into Amides Via Oximes 摘要:The Iridium Catalyst [ir(Cp*)Cl-2](2) Is Effective For The Rearrangement Of Oximes To Furnish Amides. The Reaction Has Been Combined With Catalytic Transfer Hydrogenation Between An Alcohol And Alkene To Allow The Conversion Of Alcohols Into Amides In A One-Pot Process. Doi:10.1021/ol062549U
专利号:US-6794534-B2 优先权日:2000-06-23 标题:Synthesis of functionalized and unfunctionalized olefins via cross and ring-closing metathesis 发明人:GRUBBS ROBERT H; CHATTERJEE ARNAB K; MORGAN JOHN P; SCHOLL MATTHIAS; CHOI TAE-LIM 权利人:CALIFORNIA INST OF TECHN 摘要:The invention is directed to the cross-metathesis and ring-closing metathesis reactions between geminal disubstituted olefins and terminal olefins, wherein the reaction employs a Ruthenium or Osmium metal carbene complex. Specifically, the invention relates to the synthesis of α-functionalized or unfunctionalized olefins via intermolecular cross-metathesis and intramolecular ring-closing metathesis using a ruthenium alkylidene complex. The catalysts preferably used in the invention are of the general formula n wherein: n M is ruthenium or osmium; n X and X 1 are each independently an anionic ligand; n L is a neutral electron donor ligand; and, n R, R 1 R 6 , R 7 , R 8 , and R 9 are each independently hydrogen or a substituent selected from the group consisting of C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, aryl, C 1 -C 20 carboxylate, C 1 -C 20 alkoxy, C 2 -C 20 alkenyloxy, C 2 -C 20 alkynyloxy, aryloxy, C 2 -C 20 alkoxycarbonyl, C 1 -C 20 alkylthio, C 1 -C 20 alkylsulfonyl and C 1 -C 20 alkylsulfinyl.
专利号:US-7816544-B2 优先权日:2004-03-23 标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species 发明人:JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A 权利人:UNIV BOSTON 摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-8404088-B2 优先权日:2006-05-22 标 题:Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral bronsted acids 发明人:PORCO JR JOHN A; GERARD BAUDOUIN 权利人:PORCO JR JOHN A; GERARD BAUDOUIN; UNIV BOSTON 摘要:The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
专利号:US-8951728-B2 优先权日:2004-11-22 标 题:Template directed split and mix synthesis of small molecule libraries 发明人:RASMUSSEN PETER BIRK 权利人:CHEMGENE HOLDING APS 摘要:The invention combines the advantages of split and mix synthesis with the advantages of template directed synthesis. The method comprises the steps of: a) adding a linker molecule L to one or more reaction wells; b) adding a molecule fragment to each of said reaction wells; c) adding an oligonucleotide identifier to each of said reaction wells; d) subjecting said wells to conditions sufficient to allow said molecule fragments and said oligonucleotide identifiers to become attached to said linker molecule, or conditions sufficient for said molecule fragments to bind to other molecule fragments and sufficient for said oligonucleotide identifiers to bind to other oligonucleotide identifiers; e) combining the contents of said one or more reaction wells; and f) contacting the resulting bifunctional molecule(s) of step e) with one or more (oligonucleotide) templates each capable of hybridizing to at least one of the oligonucleotide identifiers added in step c).
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-11746364-B2 优先权日:2018-01-17 标题 :Enzymatic synthesis of kavalactones and flavokavains 发明人:PLUSKAL TOMÃ?S; Weng jing-ke 权利人:WHITEHEAD INST BIOMEDICAL RES 摘要:Disclosed are methods, compositions, proteins, nucleic acids, cells, vectors, compounds, reagents, and systems for the preparation of kavalactones, flavokavains, and kavalactone and flavokavain biosynthetic intermediates using enzymes expressed in heterologous host cells, such as microorganisms or plants, or using in vitro enzymatic reactions. This invention also provides for the expression of the enzymes by recombinant cell lines and vectors. Furthermore, the enzymes can be components of constructs such as fusion proteins. The kavalactones produced can be utilized to treat anxiety disorder, insomnia, and other psychological and neurological disorders. The flavokavains produced can be utilized to treat various cancers including colon, bladder, and breast cancers.