专利号:US-3901899-A 优先权日:1973-04-27 标题 :Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an Nhaloaniline with a Beta -carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the Beta carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an Alpha -ethyl- Beta -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:US-3992392-A 优先权日:1973-04-27 标题:Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an N-haloaniline with a β-carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the β-carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an α-ethyl-β -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:US-2017355648-A1 优先权日:2016-04-26 标题 :Synthesis of meta-substituted [18f]-3-fluoro-4-aminopyridines by direct radiofluorination of pyridine n-oxides
专利号:US-10160695-B2 优先权日:2016-04-26 标 题 :Synthesis of meta-substituted [18F]-3-fluoro-4-aminopyridines by direct radiofluorination of pyridine N-oxides 发明人:BRUGAROLAS PEDRO 权利人:UNIV CHICAGO 摘要:Disclosed herein are methods for the fluorination aromatic N-heterocyclic N-oxides that comprise at least one leaving group. The N-oxides may be reduced to the fluorinated aromatic N-heterocyclic amine analogs. This novel fluorination approach may be successfully applied for synthesizing aromatic N-heterocyclic compounds labeled with 18 F.
专利号:CN-102898360-A 优先权日:2012-11-12 标题 :Synthesis of 3,5-Dibromo-4-fluoropyridine
专利号:CN-102898359-A 优先权日:2012-11-12 标题:Synthesis of 3,5-dibromo-4-iodopyridine
参考标题: Proteasome Activity Enhancing Compounds Composés Renforçant L'Activité Des Protéasomes 摘要:The Present Invention Is Directed To Compounds Having The Formula (I), (II), (III), (Iv), And (V), Compositions Thereof, The Methods Of Synthesis Of The Compouds Of Interest, And To Methods For The Treatment Of A Condition Associated With A Dysfunction In Proteostasis, Such As Cancer, Inflammatory Conditions, Neurodegeneration, Metabolic Conditions, Comprising Administering An Effective Amount Of A Compound Of The Invention.
合成参考文献
摘要:Carboni, B.; Carreaux, F., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 280. 摘要:J. M. Essery and K. Schofield. J. Chem. Soc. 1961, 3939.