专利号:US-4628123-A 优先权日:1984-10-23 标题:Process for the synthesis of 2-methoxy-6-bromo-naphthalene 发明人:BORSOTTI GIAMPIERO 权利人:MONTEDISON SPA 摘要:A process for the synthesis of 2-methoxy-6-bromo-naphthalene, wherein the 2-methoxy-naphthalene is brominated by means of Br 2 to 1,6-dibromo-2-methoxy-naphthalene and the latter is then dehalogenated, without any separation from the liquid medium of reaction, by addition of iron.
专利号:US-2025188022-A1 优先权日:2022-02-07 标 题 :Process for the preparation of nafamostat, camostat and their derivatives 发明人:AHMED RIYAZ; KUMAR GULSHAN; MAHAJAN SHEENA; Verma Praveen Kumar; CHAM PANKAJ SINGH; KUMAR AMIT; AHMED QAZI NAVEED; REDDY DUMBALA SRINIVASA; SHANKAR RAVI; SINGH PARVINDER PAL 权利人:COUNCIL SCIENT IND RES 摘要:The invention provides a novel, economical and practical route for the synthesis of an ester from acid and alcoholic functionalities using Trihalotriazine as coupling agent. Specifically, the invention provides a novel, economical and practical route for the preparation of Nafamostat and Camostat. Synthesis of p-guanidinobenzoic acid (Al) was also achieved from thiourea and p-aminobenzoic acid by using trihalotriazine as coupling reagent.
专利号:WO-2017083719-A1 优先权日:2015-11-13 标 题:Transition metal free methods of synthesis of biaryl compounds 发明人:GAO HONGYIN; KURTI LASZLO 权利人:UNIV RICE WILLIAM M 摘要:The present disclosure provides methods of preparing biaryl compounds which do not require transition metal catalysts. In yet another aspect, the present disclosure provides pharmaceutical compositions comprising compounds as described herein and pharmaceutically acceptable carriers.
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-4137272-A 优先权日:1976-05-04 标 题:Process for the manufacture of 2-alkoxy-6-bromo-naphthalenes 发明人:PAPENFUHS THEODOR; GENGNAGEL KURT 权利人:HOECHST AG 摘要:A new process, which can be carried out on the technical scale, had been found for the preparation of 2-alkoxy-6-bromo-naphthalenes, especially suitable as starting compounds for the synthesis of estrogens, which comprises brominating 2-hydroxy-naphthalene-1-carboxylic acid with bromine, decarboxylating the 6-bromo-2-hydroxynaphthalene-1-carboxylic acid by heating the reaction mixture at 100 - 125° C, and alkylating the 6-bromo-2-hydroxy-naphthalene formed. The process can be conducted easily and with high yields.
专利号:US-11718596-B2 优先权日:2014-03-19 标题 :Amyloid targeting agents and methods of using the same 发明人:YANG JERRY; THEODORAKIS EMMANUEL A; SARRAF STELLA 权利人:UNIV CALIFORNIA; AMYDIS INC 摘要:Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
[参考文献]: F Tanaka, Et Al. Visualizing Antibody-Catalyzed Retro-Aldol-Retro-Michael Reactions. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2983-6. [参考文献]: L L Spielman, Et Al. A Specific Stain For Alpha-Glucosidases In Isoelectric Focusing Gels. Anal Biochem. 1982 Feb;120(1):66-70. [参考文献]: Win-Long Chia, Et Al. A New Series Of Kinked Liquid Crystals: 2-(6-Alkoxynaphthalen-2-Yl)-6-Methoxyquinolines. Int J Mol Sci. 2015 Apr 2;16(4):7520-34.
合成参考文献
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