专利号:US-6600016-B1 优先权日:1999-08-24 标题:Multifunctionalized solid support resins for synthesis of combinatorial libraries and method for using the same 发明人:CAMPIAN EUGENE; LU BOLIANG; ZHANG JINFANG 权利人:ADVANCED SYNTECH LLC 摘要:Multifunctionalized support resin for the solid phase synthesis of combinatorial libraries is disclosed. The support resin comprises a resin backbone to which is attached a template containing at least two more attachment points which carry mutiple functionalized benzyl-type linkers. Each linker displays differing chemical stability under cleavage conditions so that products can be selectively and sequentially cleaved and separated from the reaction vessel. The linkers are independently different benzyl-type moieties, and each product synthesized on the linkers may have a different chemical structure. The support resin may further comprise an additional linker which is directly attached to the resin backbone. This linker can benzyl-type linkers or other traditional cleavable-linkers. The invention is further directed to a method for the production of mutiple combinatorial libraries in a simultaneous fashion utilizing the above described support resin. The products are selectively cleaved under conditions where only one linker site is cleaved so that the product is individually separated from the reaction vessel.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
专利号:US-9409879-B2 优先权日:2011-03-29 标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents 发明人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA 权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT 摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.
专利号:US-7566697-B2 优先权日:2002-06-10 标题 :Carboxy protection strategies for acidic C-terminal amino acids in chemical ligation of oligopeptides 发明人:BOTTI PAOLO; VILLAIN MATTEO; MANGANIELLO SONIA; GAERTNER HUBERT 权利人:AMYLIN PHARMACEUTICALS INC 摘要:The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotected acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product.
专利号:US-6583318-B2 优先权日:2001-05-17 标 题:Method for synthesis of α-sulfonamido amide, carboxylic acid and hydroxamic acid derivatives 发明人:CAMPIAN EUGENE; LOU BOLIANG; MJALLI ADNAN M M 权利人:ADVANCED SYNTECH LLC 摘要:A method of synthesizing alpha-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound alpha-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.
专利号:WO-03013740-A1 优先权日:2001-08-03 标题 :4- AND 5-AMINO-α, β UNSTATURATED ESTER SOLID SUPPORT TEMPLATES, METHOD OF PREPARATION AND FOR USING THE SAME 发明人:LOU BOLIANG; MAJJLI ADNAN M M 权利人:ADVANCED SYNTECH LLC 摘要:A substituted α, β-unsaturated ester template of the general formula (1) where: P is an insoluble substrate; n is 1 or 2; X is an atom or a functional group connecting the polymer and the linker L. having a structure such as but not limited to oxygen, ester, amide, sulfur, silicon and carbon; L is a multifunctional chemical monomer in which one functional group reacts with the polymer to form a covalent bond (X) and one other of the functional groups react with one of the R groups (R1, R2, R3, R5, or R6) through a plurality of chemical reactions to provide the desired templates for further chemistry. The ester template is useful for the solid phase synthesis of heterocycle compounds.
参考文献:10.1016/j.forsciint.2011.06.030 摘要:McDermott SD, Power JD, Kavanagh P, O'Brien J. The analysis of substituted cathinones. Part 2: an investigation into the phenylacetone based isomers of 4-methylmethcathinone and N-ethylcathinone. Forensic Sci Int. 2011 Oct 10;212(1-3):13–21. doi: 10.1016/j.forsciint.2011.06.030.