专利号:WO-2015131100-A1 优先权日:2014-02-28 标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.
专利号:US-4469895-A 优先权日:1982-10-21 标题 :Process for preparing alcohols from olefins and synthesis gas 发明人:KNIFTON JOHN F; GRIGSBY JR ROBERT A 权利人:TEXACO INC 摘要:This invention concerns an improved process of preparing predominantly linear alcohols which comprises the steps of contacting a mixture of terminal and/or internal olefins and synthesis gas with a catalyst system comprising a ruthenium-containing compound in conjunction with one or more tertiary amine promoters, dispersed in a low melting quaternary phosphonium salt and heating said resultant reaction mixture under a pressure of 100 psi or greater at a temperature of at least 50 DEG C. for a sufficient time to produce said alcohols.
专利号:US-4665222-A 优先权日:1980-01-31 标题 :Production of ethylene glycol from synthesis gas 发明人:WHYMAN ROBIN 权利人:ICI LTD 摘要:A process for the production of ethylene glycol, methanol, ethanol and/or esters thereof from mixtures of carbon monoxide and hydrogen (synthesis gas) which comprises contacting a mixture of carbon monoxide and hydrogen with a catalyst at elevated pressure in a liquid medium, said catalyst comprising ruthenium and at least one other metal from Group VIII of the Periodic Table, and wherein the molar proportion of ruthenium is at least 50 percent relative to the other Group VIII metals. The process is particularly applicable to the selective production of ethylene glycol. The preferred catalysts, which comprise ruthenium/rhodium, may be present in elemental form, as coordination compounds or salts, e.g. carbonyls, acetyl acetonates or carboxylates. It is especially preferred to use a co-catalyst comprising a compound of one or more the metals of Groups IA, IIA or IIB or a nitrogen containing cation and/or base. Suitable liquid media include carboxylic acids (e.g. acetic acid) and ethers (e.g. tetraglyme).
专利号:US-12336981-B2 优先权日:2010-09-03 标题 :Compounds and compositions for the inhibition of NAMPT 发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; DRAGOVICH Peter; GOSSELIN FRANCIS; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; ROTH BRUCE; SMITH CHASE C; WANG ZHONGGUO; YUEN PO-WAI; ZHENG XIAOZHANG 权利人:VALO HEALTH INC; GENENTECH INC 摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
专利号:WO-9948868-A9 优先权日:1998-03-26 标 题 :Heterocyclic classes of compounds for the modulating tyrosine protein kinase 发明人:FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL 权利人:SUGEN INC; UNIV NEW YORK; MAX PLANCK INST FUR BIOCHEMIE; FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL 摘要:The invention relates to certain indolinone-based and pyrazolylamide-based compounds, their method of synthesis, and combinatorial libraries consisting of the compounds. The invention also relates to methods of modulating the function of protein kinases using these compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.
专利号:WO-03055887-A1 优先权日:2001-12-21 标 题:Conjugated porphyrin, chlorin or bacteriochlorin chromophore 发明人:BOYLE ROSS WILLIAM; GREENMAN JOHN 权利人:CATALYST BIOMEDICA LTD; BOYLE ROSS WILLIAM; GREENMAN JOHN 摘要:The invention provides a porphyrin, chlorin or bacteriochlorin chromophore, which chromophore comprises one conjugating meso substituent which comprises a conjugating group Z for covalently conjugating said chromophore to a protein so as to enable delivery of the chromophore to a selected biological target in vitro or in vivo, and one, two or three hydrophilic meso substituents, wherein the hydrophilicity of the chromophore is such that either on carrying out conjugation of said chromophore to said protein by way of incubating said chromophore and said protein for one hour under standard protein conjugation conditions in 10% DMSO/water buffered to pH 9, the percentage of non-covalently bound chromophore out of total protein-bound chromophore is 5% or less; or, where said protein is bovine serum albumin, on carrying out conjugation of said chromophore to said protein by way of incubating said chromophore and said protein for one hour under standard protein conjugation conditions in 10% DMSO/water buffered to pH 9, the percentage of non-covalently bound chromophore out of total protein-bound chromophore is 20% or less. The invention further provides methods for the synthesis of such chromophores, and methods for the use of such chromophores in therapy and in analysis.