942947-94-6 + 73183-34-3 = 19798-80-2 + 944401-60-9 反应条件:1.1 Reagents: Potassium Acetate Catalysts: Dichloro[1,1′-Bis(Diphenylphosphino)Ferrocene]Palladium(Ii) Dichloromethane Addu... Solvents: 1,4-Dioxane; 6 H,115 °C 标题:Identification Of Nvp-Bkm120 As A Potent,Selective,Orally Bioavailable Class I Pi3 Kinase Inhibitor For Treating Cancer 作者:Burger,Matthew T.; Pecchi,Sabina; Wagman,Allan; Ni,Zhi-Jie; Knapp,Mark; Et Al 参考文献:Acs Medicinal Chemistry Letters 日期:2011 卷标:2(10) 页码:774-779
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-4500535-A 优先权日:1979-10-15 标 题:Method of regulating the immune response with pyridine derivatives 发明人:LOMBARDINO JOSEPH G; HARBERT CHARLES A 权利人:PFIZER 摘要:A series of 4-(2-carboxymethylthiomethyl)pyridines and related compounds, and their pharmaceutically acceptable salts, are disclosed as having immunoregulatory activity. Preferred compounds include 4-(2-carboxymethylthiomethyl)pyridine [alternatively named 2-(4-picolylthio)acetic acid] and (C 1 -C 4 )alkyl esters thereof, and 4-(1-formylmethylthiomethyl)-pyridine [alternatively named 2-(4-picolylthio)acetaldehyde] and bis(C 1 -C 4 )alkyl or cyclic acetals thereof. These acids, esters, aldehydes and acetals also have utility as intermediates in the synthesis of the corresponding 4-(2-hydroxyethylthiomethyl)pyridines.
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-0019994-A9 优先权日:1998-10-02 标题 :Estrogen receptor ligands 发明人:KATZENELLENBOGEN JOHN A; KATZENELLENBOGEN BENITA S; FINK BRIAN E; STAUFFER SHAUN R; MORTENSEN DEBORAH S; SATTIGERI VISWAJANANI JITENDRA; HUANG YING 权利人:UNIV ILLINOIS 摘要:This invention provides non-steroidal estrogen receptor ligands having a modular structure that is amenable to solid phase synthesis and the application of combinatorial synthetic methods to prepare these estrogen receptor ligands. ER ligands of this invention consist of a core scaffold that is a carbocyclic or heterocyclic-5-member ring that has two double bonds or a 6-member aromatic ring. A plurality of selected substituents are bonded to the ring substantially independently of other substituents. The modular structure of these compounds allows for synthesis of a very large numer of substituent structural variations, substituent combinations and substituent positioning on the core. The structural variants of the ER ligands of this invention exhibit a spectrum of selective affinities for ERα and ERβ and a spectrum of agonist/antagonist properties.
专利号:WO-2011050245-A1 优先权日:2009-10-23 标 题:Bicyclic heteroaryls as kinase inhibitors 发明人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS 权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS 摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.
专利号:DE-102011106849-A1 优先权日:2010-12-15 标 题:Process for the synthesis of N-N linked and around the N-N bond of rotation-inhibited bis-N-heterocyclic carbenes and their use as ligands for metal complexes
摘要:Ouali, A.; Taillefer, M., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 103. 摘要:G.B. Barlin. Unpublished data. 参考文献:10.1107/s1600536810048324 摘要:Bühler S, Schollmeyer D, Albrecht W, Laufer S. N-(4-Chloro-pyridin-2-yl)-N-(4-methyl-phenyl-sulfon-yl)acetamide. Acta Crystallogr Sect E Struct Rep Online. 2010 Nov 27;66(Pt 12):o3320. 参考文献:10.1107/s1600536810048336 摘要:Bühler S, Schollmeyer D, Albrecht W, Laufer S. N-(4-Chloro-pyridin-2-yl)-N-meth-oxy-methyl-4-methyl-benzene-sulfonamide. Acta Crystallogr Sect E Struct Rep Online. 2010 Nov 27;66(Pt 12):o3321. 参考文献:10.1016/j.cbi.2011.05.001 摘要:Jones JP, Joswig-Jones CA, Hebner M, Chu Y, Koop DR. The effects of nitrogen-heme-iron coordination on substrate affinities for cytochrome P450 2E1. Chemico-Biological Interactions. 2011 Aug;193(1):50–6. doi: 10.1016/j.cbi.2011.05.001.