专利号:US-7612229-B2 优先权日:2003-01-28 标 题:Industrial process for the synthesis of 2-substituted 1-(hydroxy-ethylidene)-1,1-bisphosfi- conic acids of high purity and the salts thereof 发明人:NEU JOZSEF; FISCHER JANOS; FODOR TAMAS; TOERLEY JOZSEF; GIZUR TIBOR; LEVAI SANDOR; DEMETER ADAM; PERENYI EVA 权利人:RICHTER GEDEON VEGYESZET 摘要:Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3′-pyridyl or 2′-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
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:US-7321044-B2 优先权日:2001-10-12 标题 :Synthesis of oxygen-substituted benzocycloheptenes as valuable intermediate products for the production of tissue-selective estrogens 发明人:PLATZEK JOHANNES; BECKMANN WOLFGANG; GEISLER JENS; KIRSTEIN HOLGER; NIEDBALLA ULRICH; OTTOW ECKHARD; RADAU SIGMAR; SCHULZ CLAUDIA; WESSA THOMAS 权利人:SCHERING AG 摘要:The invention relates to intermediate products and a new process for the production of benzocycloheptene C. n n n n n n n n n n The process for the production of its new intermediate products according to the invention starts from economical starting materials, provides the intermediate stages in high yields and high purity, without chromatographic purification steps, and allows production on an industrial scale.
专利号:US-6177572-B1 优先权日:1997-08-20 标题 :Solid and liquid-phase synthesis of benzoxazoles and benzothiazoles and their use 发明人:WANG FENGJIANG 权利人:SEPRACOR INC 摘要:Methods for preparing benzoxazoles and benzothiazoles on solid supports. Substituted benzothiazoles and benzoxazoles, libraries of the compounds, and methods of using the compounds are also disclosed.
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合成参考文献
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