专利号:US-6504041-B2 优先权日:1996-11-15 标题 :Synthesis of ruthenium or osmium metathesis catalysts 发明人:GRUBBS ROBERT H; BELDERRAIN TOMAS R; BROWN SETH N; WILHELM THOMAS E 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention relates to the synthesis of highly active ruthenium and osmium carbene metathesis catalyst in good yield from readily available starting materials. The catalysts that may be synthesized are of the general formula n wherein: n M is ruthenium or osmium; n X and X 1 are independently any anionic ligand; n L and L 1 are any neutral electron donor ligand; and, n R and R 1 are each hydrogen or one of the following substituent groups: C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkyl, 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. Optionally, the substituent group may be substituted with one or more groups selected from C 1 -C 5 alkyl, halogen, C 1 -C 5 alkoxy, and aryl. When the substitute aryl group is phenyl, it may be further substituted with one or more groups selected from a halogen, a C 1 -C 5 alkyl, or a C 1 -C 5 alkoxy. Specific synthetic protocols for vinyl alkylidene catalysts wherein R is hydrogen and R 1 is —CHCR 12 R 13 and non-vinyl alkylidene catalysts are also disclosed. In addition to the ease of synthesis (typically a one-step synthesis), the reactions generally may be run at or above room temperature and the resulting products usually may be used without extensive post synthesis purification.
专利号:US-5827794-A 优先权日:1994-02-22 标 题 :Supported highly-polar liquid phase chiral sulfonated binap catalyst for asymmetric synthesis of optically active compounds 发明人:DAVIS MARK E; WAN KAM TO 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention relates to water soluble chiral sulfonated 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl and its use as organometallic catalysts for asymmetric synthesis of optically active compounds. Asymmetric reactions of the present invention include those reactions in which organometallic catalysts are commonly used. Such reactions include, but are not limited to, reduction and isomerization reactions on unsaturated substrates and carbon--carbon bond forming reactions. Examples of such reactions include, but are not limited to, hydrogenation, hydroboration, hydrosilylation, hydride reduction, hydroformylation, alkylation, allylic alkylation, arylation, alkenylation, epoxidation, hydrocyanation, disilylation, cyclization and isomerization reactions. n The catalysts of the present invention provide the advantage of functioning in the presence of water without loss in enantioselectivity relative to the nonsulfonated BINAP catalyst in an organic solvent. As a result, the catalysts of the present invention may be employed in water, water miscible solvents, in aqueous--organic two phase solvent systems and in supported aqueous phase catalysts in organic solvents without loss in enantioselectivity. Further, the catalysts of the present invention may also be effectively employed in highly polar solvents such as primary alcohols and ethylene glycol. n The present invention also relates to a method for conducting asymmetric reactions on prochiral unsaturated bonds contained within a compound using the water soluble chiral sulfonated 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl organometallic catalysts of the present invention.
专利号:US-7820838-B2 优先权日:2002-01-29 标 题:Method for total synthesis of ecteinascidins and intermediate compounds thereof 发明人:FUKUYAMA TOHRU; KAN TOSHIYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R 2 of N 12 site is trichloroethoxycarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
专利号:US-7002017-B2 优先权日:2003-03-24 标题 :Enantioselective hydrogenation of intermediates in the synthesis of tipranavir 发明人:KLINGLER FRANZ DIETRICH; STEIGERWALD MICHAEL; EHLENZ RICHARD 权利人:BOEHRINGER INGELHEIM INT 摘要:The invention relates to a process for preparing the compounds of general formula I n nby enantioselective hydrogenation of the compounds of formula II n nin the presence of special hydrogenation catalysts. The invention is characterised by high enantioselectivity, providing easy access to a category of important pharmaceutical compositions, i.e. intermediates for the synthesis of tipranavir.
专利号:US-7399773-B2 优先权日:2001-01-09 标 题 :Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide 发明人:NELSON JADE DOUGLAS; PAMMENT MICHAEL GERARD 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.
专利号:US-7105617-B2 优先权日:2003-02-06 标题:Metal 8-hydroxyquinoline-functionalized polymers and related materials and methods of making and using the same 发明人:WECK MARCUS; MEYERS AMY 权利人:GEORGIA TECH RES INST 摘要:This invention relates to the synthesis of Mq n -containing monomeric compounds, comprising a polymerizable moiety, an Mq n -moiety, and an optional chemical spacer therebetween, wherein q, in each instance, comprises an 8-hydroxyquinoline residue, M is a metal such as Mg, Zn, Al, Ga, or In, and n is 2 or 3 as the valence of the metal requires. For example, the polymerization of Znq 2 - or Alq 3 -containing monomers, in the presence or absence of a co-monomer, provided a Znq 2 - or Alq 3 -containing polymer, which retained the optical properties of Znq 2 or Alq 3 in solution, respectively. The Mq n -containing polymers may be used in, among other things, the fabrication of light-emitting diodes (LEDs).
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