专利号:US-5849936-A 优先权日:1995-03-15 标题:Method for the synthesis of bis-tetrahydrofuranyl annonaceous acetogenins 发明人:HOYE THOMAS R; TAN LUSHI 权利人:UNIVERISTY OF MINNESOTA 摘要:A method for the synthesis of bis-tetrahydrofranyl Annonaceous acetogenins, including the natural products and analogs thereof, is provided which proceeds by the Pd-mediated coupling of a bis-tetrahydrofuranyl-subunit comprising a terminal alkyne, with a (C4)-hydroxybutenolide subunit comprising a terminal vinyl iodide, followed by selective reduction of the resulting enyne.
专利号:US-6048975-A 优先权日:1991-09-12 标 题:Process for the chemical synthesis of oligonucleotides 发明人:PFLEIDERER WOLFGANG; BERGMANN FRANK 权利人:HOECHST AG 摘要:A process for the chemical synthesis of oligonucleotides n Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. n The ease of detection of the dansyl protective group and the ease of elimination from the sugar residue of the nucleotide without side reactions make oligonucleotide synthesis possible with high yields in very small quantities.
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-2009131688-A1 优先权日:2007-11-21 标 题 :Method for the synthesis of 4-benzofuran-carboxylic acid 发明人:BURGOS ALAIN; MARUANI MARTINE; PERRIN FLORENCE; FREIN STEPHANE 权利人:ZACH SYSTEM 摘要:The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. n This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: n n n n n n n n n n wherein R independently represents hydrogen or a linear or branched C 1 - 15 alkyl group. n With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.
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-9884830-B2 优先权日:2004-05-21 标题 :Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R 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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
[参考文献]: Ali Es-Haghi, Et Al. Novel Unbreakable Solid-Phase Microextraction Fibers On Stainless Steel Wire And Application For The Determination Of Oxadiargyl In Environmental And Agricultural Samples In Combination With Gas Chromatography-Mass Spectrometry. Talanta. 2014 Oct:128:231-6.
合成参考文献
摘要:Wang, K. K., Science of Synthesis, (2008) 44, 268. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 350. 摘要:Gudat, D., Science of Synthesis Knowledge Updates, (2021) 1, 271.