专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
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-5684130-A 优先权日:1995-06-05 标题 :Process for synthesis of organic compounds using magnetic particles 发明人:SUCHOLEIKI IRVING 权利人:SOLID PHASE SCIENCES CORP 摘要:This invention provides a process for the synthesis of a defined chemical entity, i.e., any desired chemical compound, in high yield using a solid support comprising a magnetic particle, in organic solvents. In general, a sequence of chemical synthetic steps are required to prepare the defined chemical entity bound to the particle. The particle comprises a resin bearing a high concentration of substituent pendant functional groups, to which the first reagent employed in the synthetic sequence binds; in subsequent reaction steps further reagents react with the growing chemical intermediate bound to the pendant functional groups until the defined chemical entity is obtained. The particle also comprises smaller paramagnetic or superpara-magnetic particles incorporated within the resin. The magnetic particle therefore responds to imposed magnetic field gradients, permitting ease of manipulation in steps involving removal of organic solvent.
专利号:US-8754259-B2 优先权日:2008-08-15 标 题 :Synthesis of cyclohexane derivatives useful as sensates in consumer products 发明人:YELM KENNETH EDWARD; BUNKE GREGORY MARK; HAUGHT JOHN CHRISTIAN 权利人:PROCTER & GAMBLE; PROCTER & GAMBLE 摘要:The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect. Preparation schemes for neoisomers of other menthyl derivatives which are useful as coolants, including esters, ethers, carboxy esters and other N-substituted carboxamides are also provided.
专利号:US-7741492-B2 优先权日:2005-02-28 标题:Method for obtaining a pharmaceutically active compound (Irbesartan) and its synthesis intermediate 发明人:HUGUET CLOTET JOAN; DALMASES BARJOAN PERE 权利人:INKE SA 摘要:It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).
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合成参考文献
参考文献:10.1155/2011/709416 摘要:Knol RJJ, van den Bos JC, Janssen AGM, de Bruin K, van Eck-Smit BLF, Booij J. Synthesis and In Vitro Evaluation of Novel Nortropane Derivatives as Potential Radiotracers for Muscarinic M2 Receptors. International Journal of Molecular Imaging. 2011 Jun 13;2011():1–7. doi: 10.1155/2011/709416.