专利号:US-5434152-A 优先权日:1993-11-08 标题:Asymmetric synthesis of (S)-(-)-6-chloro-4- cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-quinazolinone 发明人:HUFFMAN MARK A; YASUDA NOBUYOSHI; DECAMP ANN E; GRABOWSKI EDWARD J J 权利人:MERCK & CO INC 摘要:An asymmetric synthesis of (S)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-quinazolinone comprises the chiral addition of 2-pyridylacetylide to N 1 -protected 6-chloro-4-cyclopropyl-2-quinazolinone followed by removal of the protecting group.
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:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:WO-2023203374-A1 优先权日:2022-04-20 标 题 :[1,2]selenazolo[2,3-a]pyridin-8-ium inhibitors of pyruvate kinase isoform m2 发明人:ARSENJANS PAVELS; DIMITRIJEVS PAVELS; MAKRECKA-KUKA MARINA 权利人:LATVIAN INST ORGANIC SYNTHESIS 摘要:The present invention relates to a novel isoselenazolopyridinium salts as anticancer agents by inhibiting pyruvate kinase isoform M2 (PKM2) activity, as well as methods of their manufacturing and use in different pharmaceutical compositions for the treatment of various diseases and disorders by administration of such substances.
专利号:WO-2008037604-A1 优先权日:2006-09-25 标 题 :Novel polybenzofulvene derivatives, synthesis and uses thereof 发明人:CAPPELLI ANDREA; GALEAZZI SIMONE; ANZINI MAURIZIO; VOMERO SALVATORE 权利人:UNIV SIENA; CAPPELLI ANDREA; GALEAZZI SIMONE; ANZINI MAURIZIO; VOMERO SALVATORE 摘要:The present invention relates to polymers of formula poly-3 (I), their synthesis, intermediates and uses thereof.
专利号:US-2003082830-A1 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
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合成参考文献
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