专利号:US-6603015-B2 优先权日:1999-03-29 标题:Synthesis of epothilones 发明人:GEORG GUNDA I; NAIR SAJIV K; REIFF EMILY; TUNOORI ASHOK RAO 权利人:UNIV KANSAS 摘要:Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.
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-5998633-A 优先权日:1996-07-29 标 题:Process for the synthesis of protected esters of (S)-3,4-dihydroxybutyric acid 发明人:JACKS THOMAS E; BUTLER DONALD E 权利人:WARNER LAMBERT CO 摘要:The invention is an improved process for the preparation of a compound of formula I wherein R and R 1 are each independently alkyl of from 1 to 3 carbon atoms; and R 2 is alkyl of from 1 to 8 carbon atoms. ##STR1##
专利号:US-5155251-A 优先权日:1991-10-11 标题:Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate 发明人:BUTLER DONALD E; LE TUNG V; MILLAR ALAN; NANNINGA THOMAS N 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate is described where a halo hydroxyester or other activated dihydroxyester is converted in two steps to the desired product.
专利号:US-7276598-B2 优先权日:2003-04-09 标 题:Phosphorylation reagents for improved processes to convert terminal hydroxyl groups of oligonucleotides into phosphate monoesters 发明人:VAGLE KURT; LEUCK MICHAEL; WOLTER ANDREAS 权利人:SIGMA ALDRICH CO 摘要:The present invention discloses novel phosphoramidite reagents for use in oligonucleotide synthesis. The present invention further discloses novel methods for the conversion of terminal hydroxyl groups of oligonucleotides into phosphate monoesters. By employing novel reagents, as also disclosed herein, the methods are fully compatible with standard procedures for solid phase oligonucleotide synthesis and do not require additional processing steps. The inventive reagents to phosphorylate terminal hydroxyl groups of oligonucleotides are superior to the prior art in that they for the first time combine the desired attributes of being a solid compound for facile handling, comprising two β-eliminating protective groups removable as fast or faster than the standard cyanoethyl group, providing a DMT-group for easy monitoring of the coupling efficiency, and enabling a fast final deprotection of the phosphorylated oligonucleotide without any extra manipulation steps.
专利号:US-10053483-B2 优先权日:2012-04-03 标 题 :Synthesis process of antiparasitic drug selamectin 发明人:YIN MINGXING; WU JIANCHAO; CHAI JIAN 权利人:ZHEJIANG HISUN PHARM CO LTD 摘要:Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.
参考标题:Biphasic Bioelectrocatalytic Synthesis Of Chiral β-Hydroxy Nitriles 作者:Fangyuan Dong,Hui Chen,Christian A. Malapit,Matthew B. Prater,Min Li,Mengwei Yuan,Koun Lim,Shelley D. Minteer |发布日期:2020.5.6 摘要:Nad-Dependent Dehydrogenase, The Diaphorase Modified Biocathode Was Used To Regenerate Nadh To Support The Conversion From Ethyl 4-Chloroacetoacetate (Cobe) To Ethyl (S)-4-Chloro-3-Hydroxybutanoate ((S)-Chbe) Catalyzed By Adhs. The Addition Of Methyl Tert-Butyl Ether (Mtbe) As An Organic Phase Not Only Increased The Uploading Of Cobe, But Also Prevented The Spontaneous Hydrolysis Of Cobe, Extended The Lifetime
合成参考文献
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