专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:WO-2013018053-A1 优先权日:2011-08-02 标题 :Process for the preparation of epoxides as intermediates for the synthesis of nebivolol 发明人:CIPOLLONE AMALIA; D ANDREA PIERO; FATTORI DANIELA 权利人:MENARINI INT OPERATIONS LU SA; CIPOLLONE AMALIA; D ANDREA PIERO; FATTORI DANIELA 摘要:The present invention relates to a novel process of synthesis of epoxides, 6-fluoro-2- (oxiran-2-yl) chroman (Figure 1), intermediates for the synthesis of nebivolol, depicted in Scheme (1), enabling to obtain the above- mentioned epoxides in a racemic or semichiral form.
专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:WO-9747313-A1 优先权日:1996-06-10 标题:Total synthesis of bacitracin polypetides 发明人:GRIFFIN JOHN H; MCDOUGAL PATRICK G 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Methods for the total synthesis of bacitracin-type polypeptides are described, as well as useful analogs of bacitracin A, and treatment of bacterial infection using such analogs.
专利号:US-6268534-B1 优先权日:1998-02-23 标 题 :Process for the synthesis of N,N-Dioleyl-N,N-Dimethylammonium Chloride 发明人:MATULIC-ADAMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:A novel process for the synthesis of N,N-dioleyl-N,N-dimethylammonium chloride (DODAC) is described
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).
[参考文献]: Antonio Evidente, Et Al. Sphaeropsidones, Phytotoxic Dimedone Methyl Ethers Produced By Diplodia Cupressi: A Structure-Activity Relationship Study. J Nat Prod. 2011 Apr 25;74(4):757-63. [参考文献]: Beatriz Alvarez, Et Al. Formation And Reactions Of Sulfenic Acid In Human Serum Albumin. Methods Enzymol. 2010:473:117-36. [参考文献]: Claus Jacob, Et Al. Open Season For Hunting And Trapping Post-Translational Cysteine Modifications In Proteins And Enzymes. Chembiochem. 2011 Apr 11;12(6):841-4. [参考文献]: Joseph R Burgoyne, Et Al. Contemporary Techniques For Detecting And Identifying Proteins Susceptible To Reversible Thiol Oxidation. Biochem Soc Trans. 2011 Oct;39(5):1260-7. [参考文献]: Julie A Reisz, Et Al. Thiol-Blocking Electrophiles Interfere With Labeling And Detection Of Protein Sulfenic Acids. Febs J. 2013 Dec;280(23):6150-61.
合成参考文献
参考文献:10.1107/s1600536811007318 摘要:Abdelhamid AA, Mohamed SK, Allahverdiyev MA, Gurbanov AV, Ng SW. 3,3,6,6-Tetra-methyl-9-[6-(3,3,6,6-tetra-methyl-1,8-dioxo-2,3,4,5,6,7,8,9-octa-hydro-1H-xanthen-9-yl)pyridin-2-yl]-2,3,4,5,6,7,8,9-octa-hydro-1H-xanthene-1,8-dione. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o785. 参考文献:10.1107/s1600536811008658 摘要:Mohamed SK, Abdelhamid AA, Khalilov AN, Gurbanov AV, Ng SW. 4a-Hy-droxy-3,3,6,6-tetra-methyl-9-[6-(3,3,6,6-tetra-methyl-1,8-dioxo-2,3,4,5,6,7,8,9-octa-hydro-1H-xanthen-9-yl)pyridin-2-yl]-2,3,4,4a,5,6,7,8,9,9a-deca-hydro-1H-xanthene-1,8-dione ethanol hemisolvate hemihydrate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o850–1. 参考文献:10.1107/s1600536811013481 摘要:Khalilov AN, Abdelhamid AA, Gurbanov AV, Ng SW. 9-(5-Bromo-2-hy-droxy-phen-yl)-10-(2-hy-droxy-prop-yl)-3,3,6,6-tetra-methyl-1,2,3,4,5,6,7,8,9,10-deca-hydro-acridine-1,8-dione. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1146. 参考文献:10.1007/s10895-011-0915-2 摘要:Patil SR, Shelar DP, Rote RV, Jachak MN. A fluorescence study of new angular polycyclic blue light-emitting pyrazolo[3,4-h][1,6]naphthyridine and their interaction with bovine serum albumin (BSA). J Fluoresc. 2011 Nov;21(6):2037–52. doi: 10.1007/s10895-011-0915-2. 参考文献:10.1016/j.bmc.2011.06.057 摘要:Mwakaboko AS, Zwanenburg B. Single step synthesis of strigolactone analogues from cyclic keto enols, germination stimulants for seeds of parasitic weeds. Bioorg Med Chem. 2011 Aug 15;19(16):5006–11. doi: 10.1016/j.bmc.2011.06.057.