专利号:US-6022977-A 优先权日:1997-03-26 标 题 :Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic acids 发明人:ZHANG LIN-HUA; ANZALONE LUIGI; PESTI JAAN A; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
专利号:US-10975096-B2 优先权日:2014-06-20 标题 :Synthesis of polycyclic-carbamoylpyridone compounds 发明人:CHIU ANNA; ENQUIST JR JOHN; GRIGGS NOLAN; HALE CHRISTOPHER; IKEMOTO NORIHIRO; KEATON KATIE ANN; KRAFT MATT; LAZERWITH SCOTT E; LEEMAN MICHEL; PENG ZHIHUI; SCHRIER KATE; TRINIDAD JONATHAN; VAN HERPT JOCHEM; WALTMAN ANDREW W 权利人:GILEAD SCIENCES INC 摘要:Methods of making compounds of Formula I are disclosed:
专利号:US-9834556-B2 优先权日:2014-03-24 标题 :Process of preparing 3-(3-(4-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-YL)pyridin-2-amine 发明人:BATES CRAIG; CHEN JIAN-XIE; MAO JIANMIN; REED DAVID P 权利人:ARQULE INC 摘要:The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine:
专利号:WO-2005049586-A1 优先权日:2003-11-24 标 题:Process for production of (s) -n-pentanoyl-n-[[2’-(1h-tetrazole-5yl) [1,1’-biphenyl]-4-yl]methyl]-l-valine 发明人:CEPANEC IVICA; LITVIC MLADEN; KORETIC STEFANIJA; BARTOLINCIC ANAMARIJA; DRUSKOVIC VINKA; SPOREC ANITA 权利人:BELUPO LIJEKOVI KOZMETIKA D D; CEPANEC IVICA; LITVIC MLADEN; KORETIC STEFANIJA; BARTOLINCIC ANAMARIJA; DRUSKOVIC VINKA; SPOREC ANITA 摘要:The patent relates to a new process of synthesis of an antihypertensive agent, N-pentanoyl-N-[[2'-(1H-tetrazole-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine (1), also known under the generic name of valsartan, by selective reaction of N-pentanoyl-N-[[2'-(1H-tetrazole-5-yl) [1,1'-biphenyl]-4-yl]methyl]-L-valine methyl-ester (14) with metallic or quaternary ammonium trialkylsilanolates by SN2 reaction. The compound 14 was produced in four reaction steps starting from 2N-trityl-5-(4'-methylbiphenyl-2-yl)tetrazole (17) and L-valine methyl-ester (11). Free-radical bromination of the compound 17 with N-bromosuccinimide produced 2N-trityl-5-(4'-bromomethylbiphenyl-2-yl)tetrazole (7), which in the reaction with L-valine methyl-ester (11) results in N-[[2'-(2N-trityl-tetrazole-5-yl)[1,1'-biphenyl]-4Âyl]methyl]-L-valine methyl-ester hydrobromide (15). Acylation of the compound 15 with pentanoyl chloride in the presence of trialkylamine bases results in N-pentanoyl-N-[[2'-(2NÂtrityl-tetrazole-5-yl)[1,1'-biphenyl] -4-yl]methyl]-L-valine methyl-ester (16). Removal of trityl protecting group by strong acids produces the key intermediary, compound 14.
专利号:US-4644076-A 优先权日:1985-04-11 标题:Continuous process for the synthesis of hexamethyldisilazane 发明人:FOSTER ROLAND S; ELLIS CRAIG A 权利人:FAR RESEARCH INC 摘要:A continuous process for the production of hexamethyldisilazane consisting of introducing predetermined quantities of trimethylcholorosilane and gaseous ammonia to form a mixture of hexamethyldisilazane and ammonium chloride in a first reactor, while simultaneously subjecting said mixture to continuous high shear agitation to form a slurry, and then separating the ammonia choloride from said slurry to provide a solution principally comprising hexamethyldisilazane and apparatus useful with the foregoing process.
专利号:WO-2024227071-A1 优先权日:2023-04-26 标 题:Synthesis of durlobactam 发明人:RIBE SETH 权利人:ENTASIS THERAPEUTICS LTD; RIBE SETH 摘要:Provided herein are methods of preparing durlobactam sodium and durlobactam tributylammonium salts.
摘要:Tius, M. A., Science of Synthesis Knowledge Updates, (2022) 1, 456. 摘要:Couve-Bonnaire, S.; Castanheiro, T.; Bouillon, J.-P., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2. 摘要:Semeniuk, T.; Hamel, J.-D., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.