专利号:US-4910310-A 优先权日:1988-10-03 标 题:Synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives 发明人:CAMPBELL ARTHUR L; BEHLING JAMES R; BABIAK KEVIN A; NG JOHN S; MUELLER RICHARD A; FLEET GEORGE W J 权利人:SEARLE & CO 摘要:Novel intermediates and method for the chemical synthesis of N-substituted 1,5-dideoxy-1,5-imino-L-fucitol derivatives are provided. A preferred intermediate is 1,5-dideoxy-1,5-imino-3, 4-O-isopropylidene-L-fucitol which is used to prepare the HIV inhibitor 1,5-dideoxy-1,5-imino-[N-ω-methyl caproate]-L-fucitol. These compounds are prepared in a short synthesis from the known compound 2,3-O-isopropylidene-D-lyxono-1,4-lactone or in a multi-step synthesis from D-galactose.
专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-11059914-B2 优先权日:2016-12-21 标题:Method for the continuous synthesis of a diene elastomer with lithium amide initiator 发明人:DIRE CHARLOTTE; DESSENDIER MARIE-HÉLÈNE 权利人:MICHELIN & CIE 摘要:A process for the continuous synthesis of a diene elastomer is provided. The synthesis is conducted by means of n reactors r1 to rn, considered to be continuous stirred-tank reactors, which are equipped with an internal stirring system. The reactors are arranged in series, n varying from 2 to 15, preferably from 2 to 9. The reactor r1 is fed by an input solution comprising a solvent, one or more monomer(s), an anionic polymerization initiator chosen from lithium amides and a polar agent. The conversion by weight C1 in the first reactor is less than 70%, and the total conversion by weight Cn at the outlet of the reactor rn is greater than or equal to 70%.
专利号:US-2024067694-A1 优先权日:2021-01-04 标 题:Synthesis of teduglutide 发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR 权利人:BIOCON LTD 摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.
专利号:US-2024400517-A1 优先权日:2022-02-08 标 题 :Chiral bimetallic cooperative catalysis system and use thereof in asymmetric synthesis of bedaquiline 发明人:ZHANG WANBIN; GAO FENG; LI JING; AHMAD TANVEER; ZHANG ZHENFENG; YUAN QIANJIA 权利人:UNIV SHANGHAI JIAOTONG 摘要:A chiral bimetallic cooperative catalysis system and use thereof in asymmetric synthesis of bedaquiline are provided. Specifically, the chiral bimetallic cooperative catalysis system is formed by a metallic lithium, sodium or potassium salt and another metal salt under the action of a suitable ligand and an additive. By means of the chiral bimetallic cooperative catalysis system, an addition reaction of 6-bromo-3-benzyl-2-methoxyquinoline (I) and 3-dimethylamino-1-naphthyl-1-propanone (II) is promoted, the selectivity is regulated, and a target product, (1R,2S)-bedaquiline, with high yield and high selectivity is obtained for the first time.
参考标题:&agr;-Aminoboronic Acids Prepared By Novel Synthetic Methods 摘要:The Present Invention Relates To A Novel Class Of &agr;-Aminoboronic Acids Of Formula (V), Which Are Useful As Intermediates In Synthetic Processes For Inhibitors Of The Serine Proteases, Leukocyte Elastase, Pancreatic Elastase, Cathepsin G, And Chymotrypsin. More Specifically, The &agr;-Aminoboronic Acids Are Useful As Intermediates For The Synthesis Of Hepatitis C Virus (Hcv) Protease Inhibitors. This Invention Also Generally Relates To Novel Methods For The Preparation Of &agr;-Aminoboronic Acids.
合成参考文献
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