专利号:US-7893286-B2 优先权日:2007-06-01 标题 :Method for the synthesis of phospholipid ethers 发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC 权利人:CELLECTAR INC 摘要:Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.
专利号:US-6603070-B2 优先权日:2000-07-21 标题 :Convergent synthesis of multiporphyrin light-harvesting rods 发明人:LINDSEY JONATHAN S; LOEWE ROBERT S 权利人:UNIV NORTH CAROLINA STATE 摘要:The present invention provides a convergent method for the synthesis of light harvesting rods. The rods are oligomers of the formula A 1 (A b+1 ) b , wherein b is at least 1, A 1 through A b+1 are covalently coupled rod segments, and each rod segment A 1 through A 1+b comprises a compound of the formula X 1 (X m+1 ) m wherein m is at least 1 and X 1 through X m+1 are covalently coupled porphyrinic macrocycles. Light harvesting arrays and solar cells containing such light harvesting rods are also described, along with intermediates useful in such methods and rods produced by such methods.
专利号:US-6780810-B2 优先权日:2002-03-13 标题:Multifunctional catalyst useful in the synthesis of chiral vicinal diols and process for the preparation thereof, and process for the preparation of chiral vicinal diols using said multifunctional catalysts 发明人:CHOUDARY BOYAPATI MANORANJAN; CHOWDARI NAIDU SREENIVASA; MADHI SATEESH; KANTAM MANNEPALLI LAKSHMI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a multifunctional reusable catalyst and to a process for the preparation thereof on a single matrix of the support to perform multicomponent reaction in a single pot. The multifunctional catalysts of the invention are useful for the synthesis of chiral vicinal diols by tandem and/or simultaneous reactions involving Heck coupling, N-oxidation and AD reaction of olefins in presence of cinchona alkaloid compounds both as an native one and immobilized one in the said matrix support. This invention also relates to a process for preparing vicinal diols by asymmetric dihydroxylation of olefins in presence of cinchona alkaloid compounds employing reusable multifunctional catalysts as heterogeneous catalysts in place of soluble osmium catalysts.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:EP-1641729-B1 优先权日:2003-07-09 标题:Use of functionalized onium salts as a soluble support for organic synthesis 发明人:VAULTIER MICHEL; GMOUH SAID; HASSINE FATIMA 权利人:CENTRE NAT RECH SCIENT; UNIV RENNES 摘要:The invention relates to the use of a onium salt functionalized by at least one organic function, as a soluble support, in the presence of at least one organic solvent, for organic synthesis of a molecule, in a homogenous phase, by at least one transformation of said organic function. The onium salt enables the synthesized molecule to be released. The onium salt is present in liquid or solid form at room temperature and corresponds to formula A1+, X1-, wherein A1+ represents a cation and X1- represents an anion.
专利号:US-9018371-B2 优先权日:2007-03-07 标 题 :Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient 发明人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH 权利人:JEONG LAK SHIN; KIM HEA OK; JACOBSON KENNETH A; CHOE SEUNG AH; FM THERAPEUTICS CO LTD; US OF AMERICA AS REPRESENTED BY THE SECRETARY DEPT OF HEALTH AND HUMAN SERVICES THE OFFICE OF TECHNO 摘要:Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A 3 adenosine receptors and act as A 3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
[参考文献]: Eiji Shirakawa, Et Al. Mizoroki-Heck-Type Reaction Mediated By Potassium Tert-Butoxide. Angew Chem Int Ed Engl. 2011 May 9;50(20):4671-4. [参考文献]: V I Sokolov, Et Al. [参考文献]: Gig Tr Prof Zabol. 1992:(9-10):44-5. [参考文献]: Zheng-Hui Guan, Et Al. Palladium-Catalyzed Synthesis Of Indene Derivatives Via Propargylic Carbonates With In Situ Generated Organozinc Compounds. Org Biomol Chem. 2008 Mar 21;6(6):1040-5.
合成参考文献
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