专利号:US-6448058-B1 优先权日:1997-09-12 标 题:Methods for solid phase synthesis of mercapto compounds and derivatives, combinatorial libraries thereof and compositions obtained thereby 发明人:PATEL DINESH V; NGU KHEHYONG; ZHOU JIANPING 权利人:VERSICOR INC 摘要:Methods of preparing combinatorial libraries of mercapto (thiol) compounds them and compositions obtained therefrom are disclosed. The compounds are synthesized on a solid support. Following synthesis, the compounds are optionally cleaved from the support. One such method of synthesis involves attack of an S-protected nucleophile on a resin functionalized with a leaving group. The invention also provides for screening the mercapto compounds for bioactive compounds; in particular, for inhibitors of MMPs.
专利号:US-2014309424-A1 优先权日:2011-06-30 标题:Direct synthesis of 18f-fluoromethoxy compounds for pet imaging and the provision of new precursors for direct radiosynthesis of protected derivatives of o-([18f] fluoromethyl) tyrosine 发明人:BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN 权利人:BRUMBY THOMAS; GRAHAM KEITH; KRUGER MARTIN; PIRAMAL IMAGING SA 摘要:The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18 F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([ 18 F]Fluoromethyl)tyrosines.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-9045381-B2 优先权日:2010-10-19 标 题:Ruthenium complexes and their uses in processes for formation and/or hydrogenation of esters, amides and derivatives thereof 发明人:MILSTEIN DAVID; BALARAMAN EKAMBARAM; GUNANATHAN CHIDAMBARAM; GNANAPRAKASAM BOOPATHY; ZHANG JING 权利人:MILSTEIN DAVID; BALARAMAN EKAMBARAM; GUNANATHAN CHIDAMBARAM; GNANAPRAKASAM BOOPATHY; ZHANG JING; YEDA RES & DEV 摘要:The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to the novel uses of certain pyridine Ruthenium catalysts.
专利号:US-7056348-B2 优先权日:2001-04-19 标题:5-aryl-1,3,3-trimethyl-2-methylene-indoline derivatives and salts thereof, methods for the production and use of said compounds for the temporary coloration of fibers 发明人:SAUTER GUIDO; BRAUN HANS-JUERGEN; REICHLIN NADIA 权利人:WELLA AG 摘要:A method for the synthesis of 5-aryl-1,3,3,-trimethyl-2-methylene-indoline derivatives of Formula (I) or its salts of Formula (Ia) wherein 1 mole of a 5-aryl-2,3,3-trimethyl-3H-indole derivative of Formula (VII) is reacted for 1 to 44 hours at a temperature of 20° to 180° C. in an apolar, aprotic or polar, protic or polar aprotic solvent with 1 to 50 moles of a compound of Formula R1-A; new compounds of Formulas (I)/(Ia) and (V), obtainable by this method as well as an agent containing at least one compound of Formula (I)/(Ia) and a carbonyl/imine compound for dyeing keratinic fibers and a method for temporarily dyeing keratin fibers, for which the keratin fiber is dyed with the aforementioned agent and the dyeing, so obtained, is removed again at any later time by a sulfite preparation.
专利号:US-11420997-B2 优先权日:2018-04-13 标题:Peptide synthesis method 发明人:SUZUKI HIDEAKI; MUTO SUSUMU; FUJITA SHUJI; KUBO DAISUKE 权利人:JITSUBO CO LTD 摘要:The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis. Provided is the peptide synthesis method that includes the following steps a-d: step a: a carrier-protected amino acid, carrier-protected peptide, or a carrier-protected amino acid amide, and an N-Fmoc-protected amino acid or an N-Fmoc-protected peptide are condensed in an organic solvent or a mixed solution of organic solvents, to obtain an N-Fmoc-carrier-protected peptide, step b: a water-soluble amine is added to the reaction solution after the condensation reaction, step c: the Fmoc group is deprotected from the protected amino group in the presence of a water-soluble amine, and step d: the reaction solution is neutralized by adding an acid, and further, by adding and washing with an acidic aqueous solution, then, by liquid-liquid separation an aqueous layer is removed to obtain an organic layer.
[参考文献]: Marie Couturier, Et Al. Characterization Of A New Aryl-Alcohol Oxidase Secreted By The Phytopathogenic Fungus Ustilago Maydis. Appl Microbiol Biotechnol. 2016 Jan;100(2):697-706.
合成参考文献
摘要:Sankararaman, S., Science of Synthesis, (2008) 43, 458. 参考文献:10.1007/s00253-015-7021-3 摘要:Couturier M, Mathieu Y, Li A, Navarro D, Drula E, Haon M, Grisel S, Ludwig R, Berrin JG. Characterization of a new aryl-alcohol oxidase secreted by the phytopathogenic fungus Ustilago maydis. Appl Microbiol Biotechnol. 2016 Jan;100(2):697–706. doi: 10.1007/s00253-015-7021-3. 参考文献:10.1007/s11030-005-8104-3 摘要:Chen CH, Zhang W. Fluorous reagents and scavengers versus solid-supported reagents and scavengers, a reaction rate and kinetic comparison. Molecular Diversity. 2005 Nov;9(4):353–9. doi: 10.1007/s11030-005-8104-3.