专利号:US-2025179020-A1 优先权日:2023-12-05 标 题:Synthesis of bis-oxime heterocycles 发明人:BLUMBERG SHAWN T; DORSEY CHRISTOPHER L 权利人:SOUTHWEST RES INST 摘要:A synthesis of bis-oxime heterocycles via reaction of 2,4-dimethyl pyridine or 2,4-dimethylpyrimidine in the presence of a phase transfer catalyst. Such bis-oxime heterocycles provide a more direct route to the synthesis of bis-quaternary pyridinium compounds and their analogs as nerve agent antidotes.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:WO-0168615-A1 优先权日:2000-03-13 标题 :Quinazoline synthesis 发明人:DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT 权利人:CHEMRX ADVANCED TECHNOLOGIES I; DENER JEFFREY MARK; LEASE TIMOTHY G; NOVACK AARON ROBERT 摘要:The present invention relates to a method for making a compound of Formulas I, II and III. The method of the present invention also enables parallel and simultaneous synthesis of a plurality of compounds represented by Formulas I, II and III.
专利号:US-6734309-B1 优先权日:2002-12-23 标题:Process for the synthesis of isonicotinic acid hydrazide 发明人:RAY SUBHASH CHANDRA; NANDI LAKSHMI NARAYAN; SINGH BALDEV; PRASAD HIRALAL; MAHARAJ SUMANT; SARKAR PRODYOT KUMAR; DUTTA PASHUPATI; ROY SHYAM KISHORE; YADAV SATYA NIKETAN; BANDYOPADHYAY ANUP KUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The invention provides a process for the manufacture of isonicotinic acid hydrazide(INH) useful in the treatment of tuberculosis. The invention relates to the single step conversion of isonicotinamide by hydrazine hydrate to isonicotinic acid hydrazide (INH) of yield greater than 95% (w/w) and purity more than 99%.
专利号:US-8524782-B2 优先权日:2008-07-23 标题 :Key intermediate for the preparation of Stilbenes, solid forms of Pterostilbene, and methods for making the same 发明人:SUBBARAJU GOTTUMUKKALA V; MAHESH MASNA; MOHAN HINDUPUR R; SURESH THATIPALLY; IVANISEVIC IGOR; ANDRES MARK; STEPHENS KYLE 权利人:SUBBARAJU GOTTUMUKKALA V; MAHESH MASNA; MOHAN HINDUPUR R; SURESH THATIPALLY; IVANISEVIC IGOR; ANDRES MARK; STEPHENS KYLE; LAURUS LABS PRIVATE LTD 摘要:The present invention provides a scalable process for the preparation of stilbenes by (i) condensing 3,5-dialkylbenzyl phosphonates with 4′-O-tetrahydropyranyl benzaldehyde to get 3,5-alkyl-4′-O-tetrahydropyranyl Stilbene and (ii) deprotecting the obtained 3,5-Dialkyl-4′-O-tetrahydropyranylstilbene to yield stilbenes. The present invention also provides a novel intermediate 3,5-Dialkyl-4′-O-tetrahydropyranyl stilbene, which is a key intermediate for the synthesis of stilbenes such as Pterostilbene and Resveratrol. The present invention also provides characteristics of various solid forms of Pterostilbene, methods for their preparation, as well as dosage forms containing the same for administration to or consumption by humans.
专利号:US-9549917-B2 优先权日:2011-09-08 标 题 :Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS; MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
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