专利号:US-9920084-B2 优先权日:2011-08-23 标题 :Ionic tags for synthesis of oligoribonucleotides 发明人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK-HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER 权利人:DAMHA MASAD J; HASSLER MATTHEW; CHAN TAK HANG; NANDYALA MALLIKARJUNA REDDY; DONGA ROBERT ALEXANDER; THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIV; HONG KONG POLYTECHNIC UNIV 摘要:The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.
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-2024294462-A1 优先权日:2023-02-15 标题:Method for the Synthesis of Ionizable Lipids Using a Doubly Alkylated Intermediate 发明人:SAADATI FARIBA; TRAN HUY; CIUFOLINI MARCO; ATMURI N D PRASAD 权利人:NANOVATION THERAPEUTICS INC 摘要:Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:US-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
[参考文献]: Junya Ito, Et Al. Direct Separation Of The Diastereomers Of Phosphatidylcholine Hydroperoxide Bearing 13-Hydroperoxy-9Z,11E-Octadecadienoic Acid Using Chiral Stationary Phase High-Performance Liquid Chromatography. J Chromatogr A. 2015 Mar 20:1386:53-61.
合成参考文献
摘要:Schramm, M. P., Science of Synthesis, (2009) 46, 448. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 851. 摘要:Fringuelli, F.; Piermatti, O.; Pizzo, F.; Vaccaro, L., Science of Synthesis, (2010) 47, 619. 摘要:Zaidlewicz, M.; Krzemiński, M. P.; Dzieleńdziak, A., Science of Synthesis, (2009) 48, 366. 摘要:Takeda, T.; Tsubouchi, A., Science of Synthesis, (2009) 46, 69.