5-甲基-2-己酮肟置于盐酸,Sodium Chlorite体系中,用 水 用作溶剂,化学反应 0.08H,以92%的收率获得5-甲基-2-己酮 参考文献:A Rapid,Efficient Method For Deprotection Of Oximes To Carbonyl Compounds With Naclo2<> In Water 标题:A Rapid,Efficient Method For Deprotection Of Oximes To Carbonyl Compounds With Naclo2<> In Water 摘要:一种利用水中的次氯酸钠(naclo2)对肟进行快速,高效的脱保护以得到羰基化合物的方法已被展示.该方案已被发现适用于广泛的醛肟和酮肟,且能够以非常好至优秀的收率获得相应的羰基化合物. Doi:10.2174/157017861201150112125024
专利号:WO-2009135600-A1 优先权日:2008-05-07 标题:Catalysts for the synthesis of polyurethanes 发明人:LINDNER STEFAN; BAHNMUELLER STEFAN; SCHMIDT AXEL; WEIKARD JAN; BUCHMEISER MICHAEL; BANTU BHASKER; FRIEDERICHS WOLFGANG; KRAUSE JENS; REITER STEPHAN 权利人:BAYER MATERIALSCIENCE AG; LINDNER STEFAN; BAHNMUELLER STEFAN; SCHMIDT AXEL; WEIKARD JAN; BUCHMEISER MICHAEL; BANTU BHASKER; FRIEDERICHS WOLFGANG; KRAUSE JENS; REITER STEPHAN 摘要:The invention relates to novel catalysts for the synthesis of polyurethanes, represented by general formula (I) or (II), or compounds obtained by reacting a metal salt of the metals magnesium, calcium, yttrium, lanthanum, titanium, zirconium, manganese, iron, cobalt, zinc, aluminium, tin, comprising an anion from the group fluoride, chloride, bromide, sulphonate, trifluoromethanesulphonate, methanesulphonate, benzolsulphonate, para-toluenesulphonate, carboxy-C1-C10-alkyl, carboxy-C3-C10-cycloalkyl, carboxy- C2-C10-alkenyl, C1-C10-alkoxy, acetylacetonate, trifluoroacetlyacetonate or hexafluoroacetylacetonate, with N-heterocyclic compounds of general structure I; or with N-heterocyclic compounds of general structure II; or with N-heterocyclic compounds of general structure III.
专利号:US-10905769-B2 优先权日:2015-11-13 标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI 权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:WO-2025073833-A1 优先权日:2023-10-04 标 题:Optimized process for the preparation of iopamidol 发明人:BUONSANTI FEDERICA; MAZZON ROBERTA; FRETTA ROBERTA 权利人:BRACCO IMAGING SPA 摘要:The present invention relates to the field of organic chemistry, in particular to the synthesis of iodinated contrast agents. More in particular, the invention relates to a sustainable process for the synthesis of iopamidol which allows to improve the purity profile of the product and avoids the use of potentially hazardous reagents and solvents.
专利号:US-7820858-B2 优先权日:2006-03-25 标 题 :Concise β2-amino acid synthesis via organocatalytic aminomethylation 发明人:CHI YONGGUI; GELLMAN SAMUEL H; POMERANTZ WILLIAM C; HORNE WILLIAM S; GUO LI; ENGLISH EMILY P 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides a method for the synthesis of β 2 -amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β 2 -amino acids.
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
参考标题:Organocatalyzed Kabbe Condensation Reaction For Mild And Expeditious Synthesis Of 2,2‐dialkyl And 2‐spiro‐4‐chromanones 作者:Naval P. Kapuriya,Jasmin J. Bhalodia,Mrunal A. Ambasana,Rashmi B. Patel,Atul H. Bapodra 摘要:An Expeditious Kabbe Condensation Reaction For The Synthesis Of 2,2‐dialkyl And 2‐spiro‐chroman‐4(1H)‐ones Has Been Developed Using Pyrrolidine‐butanoic Acid In Dmso As Bifunctional Organocatalyst. Unlike Existing Methods, This Reaction Proceeds At Room Temperature With High Yields, Rendering It An Attractive Method To Synthesize A Vast Variety Of Privileged 4‐chromones.
合成参考文献
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