专利号:US-5256799-A 优先权日:1992-07-14 标 题 :Preparation of 6-hydroxyindolines and their use for preparation of novel laser dyes 发明人:FIELD GEORGE F; HAMMOND PETER R 权利人:US OF AMERICAS AS REPRESENTED 摘要:A novel method for the synthesis of 6-hydroxyindolines and new fluorescent dyes produced therefrom, which dyes are ring-constrained indoline-based rhodamine class dyes. These dyes have absorption and emission spectra which make them particularly useful in certain dye laser applications.
专利号:US-9533959-B2 优先权日:2013-10-07 标 题:Methods of regioselective synthesis of 2,4-disubstituted pyrimidines 发明人:CHARRIER JEAN-DAMIEN; O'DONNELL MICHAEL EDWARD 权利人:VERTEX PHARMA 摘要:The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.
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:WO-2023098592-A1 优先权日:2021-11-30 标题:Preparation method for carbon-loaded iron-based catalyst and use thereof in synthesis of intermediates of anti-cancer inhibitors
专利号:CN-114315595-B 优先权日:2021-11-30 标题 :Preparation method of a carbon-supported iron-based catalyst and its application in the synthesis of anti-cancer inhibitor intermediates
[参考文献]: Maria Grazia Ferlin, Et Al. Synthesis And In Vitro And In Vivo Antitumor Activity Of 2-Phenylpyrroloquinolin-4-Ones. J Med Chem. 2005 May 5;48(9):3417-27.
合成参考文献
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 213. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 216.