N-Methyl-3-(Tritylthio)-Maleimide置于dl-Dithiothreitol,三乙胺体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 0.25H,以96%的收率获得产物三苯甲硫醇 参考文献:A Mild And Selective Protecting And Reversed Modification Of Thiols 标题:A Mild And Selective Protecting And Reversed Modification Of Thiols 摘要:One Selective Thiol-Protecting Study Has Been Investigated For A Wide Range Of Thiols Including General Thiols And Thiols Containing Multiple Functional Groups. The Reactions Of Bromomaleimides And Thiols Under The Mild Condition Afforded The Protected Products In Excellent Yields. The Thiols Can Be Recovered Very Quickly Using Dithiothreitol (Dtt) Under The Mild Condition. (C) 2016 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tetlet.2016.05.027
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-11370736-B2 优先权日:2019-04-01 标 题:Synthesis of fluoro hemiacetals via transition metal-catalyzed fluoro ester and carboxamide hydrogenation 发明人:DUB PAVEL A; BATRICE RAMI J; GORDON JOHN C 权利人:TRIAD NAT SECURITY LLC 摘要:This application is directed to use of transition metal-ligand complexes to hydrogenate fluorinated esters and carboxamides into fluorinated hemiacetals. Methods for synthesis of certain ligands are also provided.
专利号:US-4783529-A 优先权日:1985-12-03 标题 :Rapid synthesis of radiolabeled porphyrin complexes for medical application 发明人:LAVALLEE DAVID K; MANSUY DANIEL; BATTIONI JEAN-PAUL 权利人:RES CORP TECHNOLOGIES INC 摘要:This invention relates to a novel method for the rapid synthesis of radiolabeled porphyrin complexes which are highly useful for biomedical application, i.e. conjugation to protein antibodies for use in tumor imaging and internal radiation therapy.
专利号:WO-9915510-A1 优先权日:1997-09-24 标 题:Protecting and linking groups for organic synthesis 发明人:TOTH ISTVAN; DEKANY GYULA; KELLAM BARRY 权利人:ALCHEMIA PTY LTD; TOTH ISTVAN; DEKANY GYULA; KELLAM BARRY 摘要:This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups which are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis. In its most general aspect, the invention provides a cyclic compound of general formula (I).
专利号:US-6765089-B1 优先权日:1997-09-24 标 题 :Protecting and linking groups for organic synthesis on solid supports 发明人:TOTH ISTVAN; DEKANY GYULA; KELLAM BARRY 权利人:ALCHEMIA PTY LTD 摘要:This invention relates to methods for synthesis of organic compounds, and in particular to compounds useful as protecting and linking groups for use in the synthesis of peptides, oligosaccharides, glycopeptides and glycolipids. The invention provides protecting and linking groups that are useful in both solid phase and solution synthesis, and are particularly applicable to combinatorial synthesis.
专利号:US-2005014954-A1 优先权日:2001-11-22 标 题:Pyrrole synthesis 发明人:OHRLEIN REINHOLD; BAISCH GABRIELE 摘要:The invention relates to a novel process for the preparation of N-substituted pyrroles, especially of formula (V), wherein the radicals are as defined in the description, by intermolecular aza-Wittig reaction starting from organic azides and 1,4-dioxo compounds. The invention relates also to novel iminophosphorane intermediates for this synthesis. The resulting pyrroles are useful, for example, in the organic synthesis of pharmaceuticals or other active substances and chemicals.
[参考文献]: Salvatore Debonis, Et Al. Structure-Activity Relationship Of S-Trityl-L-Cysteine Analogues As Inhibitors Of The Human Mitotic Kinesin Eg5. J Med Chem. 2008 Mar 13;51(5):1115-25.
合成参考文献
参考文献:10.1107/s1600536811014929 摘要:Neuba A, Flörke U, Henkel G. N-[Bis(dimethyl-amino)-methyl-idene]-2-[(triphenyl-meth-yl)sulfan-yl]ethanaminium hexa-fluoro-phosphate. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1238–9.