专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
专利号:US-2007049757-A1 优先权日:2005-08-26 标题:Methods for the synthesis of substituted amino uracils 发明人:RIEGER JAYSON M; THOMPSON ROBERT 权利人:RIEGER JAYSON M; THOMPSON ROBERT 摘要:The invention provides novel methods of preparing substituted amino uracil compounds that can be employed as useful intermediates in the synthesis of various xanthines. Highly regioselective unsymmetrical amino uracils can be obtained using these methods which is a particular advantage over other existing methods.
专利号:US-10538790-B2 优先权日:2016-04-04 标题 :Bioenzymatic synthesis of THC-v, CBV and CBN and their use as therapeutic agents 发明人:KAVARANA MALCOLM J; PEET RICHARD C 权利人:TEEWINOT TECH LIMITED 摘要:The present invention provides methods for producing cannabinoids. More specifically, the invention is directed to the bio-enzymatic synthesis of THC-v, CBV and CBN by contacting a compound according to Formula I with a cannabinoid synthase enzyme. Also described is a system for producing these pharmaceutically important cannabinoids and the use of such cannabinoids as therapeutic agents.
专利号:US-9221821-B2 优先权日:2012-06-05 标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds 发明人:DIEP NHUT; KALYAN YURIY B 权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD 摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
专利号:US-10829792-B2 优先权日:2017-03-21 标 题 :Biocatalytic synthesis of strained carbocycles 发明人:CHEN KAI; HUANG XIONGYI; KAN S B JENNIFER 权利人:CALIFORNIA INST OF TECHN 摘要:Provided herein are methods for producing products containing strained carbocycles, such as cyclopropene moieties and/or bicyclobutane moieties. The methods include combining an alkyne and a carbene precursor in the presence of a heme protein, e.g., a cytochrome P450, under conditions sufficient to form the strained carbocycle. Reaction mixtures for producing strained carbocycles are also described, as well as whole-cell catalysts comprising heme proteins and variants thereof for forming cyclopropenes, bicyclobutanes, and related products.
专利号:US-9988349-B2 优先权日:2014-01-03 标 题:Direct stereospecific synthesis of unprotected aziridines from olefins 发明人:ESS DANIEL HALSELL; FALCK JOHN RUSSELL; JAT JAWAHAR LAL; KURTI LASZLO 权利人:ESS DANIEL HALSELL; FALCK JOHN RUSSELL; JAT JAWAHAR LAL; KURTI LASZLO 摘要:A method for the direct stereospecific conversion of structurally diverse mono-, di-, tri- and tetra-substituted olefins to N—H, N-alkyl, N-cycloalkyl, or N-aralkyl aziridines using a hydroxylamine amination agent with transition metal catalyst. The method is operationally simple (i.e., one-pot), scalable and fast at ambient temperature.
参考标题:A Palladium-Catalyzed Multi-Component Annulation Approach Towards The Synthesis Of Phenanthrenes 作者:Juan Song,Songjiang Wang,Haisen Sun,Yuxuan Fan,Kang Xiao,Yan Qian 摘要:Palladium-Catalyzed Three-Component Cascade Reaction Has Been Developed For The Facile Construction Of Phenanthrene Frameworks. The Transformation Is Driven By A Controlled Reaction Sequence Of Suzuki-Miyaura Coupling Followed By The Insertion Of Alkynes, And Finally, Annulation To Yield Phenanthrene Derivatives Via C-H Activation. This Methodology Is Able To Accommodate A Variety Of Substrates And Affords
合成参考文献
摘要:Negishi, E.; Wang, G., Science of Synthesis, (2010) 47, 925. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 189. 摘要:Kwiatkowska, M.; Kiełbasiński, P., Science of Synthesis: Knowledge Updates, (2024) 3, 417. 摘要:Lin, Z.; Tao, R.; Zhao, Y., Science of Synthesis: Knowledge Updates, (2023) 1, 385.