- Palladium-catalyzed c(sp2)-n bond cross-coupling with triaryl phosphates
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The first general palladium-catalyzed amination of aryl phosphates is described. The combination of MorDalPhos with [Pd(-cinnamyl)Cl]2 enables the amination of electron-rich, electron-neutral, and electron-poor aryl phosphates with a board range of aromatic, aliphatic, and heterocyclic amines. Common functional groups such as ether, keto, ester, and nitrile show an excellent compatibility in this reaction condition. The solvent-free amination reactions are also successful in both solid coupling partners. The gram-scale cross-coupling is achieved by this catalytic system.
- Chen, Zicong,Chen, Xiangmeng,So, Chau Ming
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- Palladium-Catalyzed C(sp2)-N Bond Cross-Coupling with Triaryl Phosphates
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The first general palladium-catalyzed amination of aryl phosphates is described. The combination of MorDalPhos with [Pd(?-cinnamyl)Cl]2 enables the amination of electron-rich, electron-neutral, and electron-poor aryl phosphates with a board range of aromatic, aliphatic, and heterocyclic amines. Common functional groups such as ether, keto, ester, and nitrile show an excellent compatibility in this reaction condition. The solvent-free amination reactions are also successful in both solid coupling partners. The gram-scale cross-coupling is achieved by this catalytic system.
- Chen, Zicong,Chen, Xiangmeng,So, Chau Ming
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p. 6366 - 6376
(2019/05/24)
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- Robust Buchwald-Hartwig amination enabled by ball-milling
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An operationally simple mechanochemical method for the Pd catalysed Buchwald-Hartwig amination of arylhalides with secondary amines has been developed using a Pd PEPPSI catalyst system. The system is demonstrated on 30 substrates and applied in the context of a target synthesis. Furthermore, the performance of the reaction under aerobic conditions has been probed under traditional solution and mechanochemical conditions, the observations are discussed herein.
- Cao, Qun,Nicholson, William I.,Jones, Andrew C.,Browne, Duncan L.
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supporting information
p. 1722 - 1726
(2019/02/20)
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- NOVEL 5 or 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS SELECTIVE INHIBITORS OF INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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Disclosed herein are 5 or 8-substituted imidazo [1, 5-a] pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo [1, 5-a] pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8-substituted imidazo [1, 5-a] pyridines that can be useful for inhibiting indoleamine 2, 3-dioxygenase and/or tryptophane 2, 3-dioxygenase and for treating diseases or disorders mediated thereby.
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Paragraph 0390; 0391
(2018/04/20)
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- Dual C(sp3)?H Bond Functionalization of N-Heterocycles through Sequential Visible-Light Photocatalyzed Dehydrogenation/[2+2] Cycloaddition Reactions
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Herein we describe a mild method for the dual C(sp3)?H bond functionalization of saturated nitrogen-containing heterocycles through a sequential visible-light photocatalyzed dehydrogenation/[2+2] cycloaddition procedure. As a complementary approach to the well-established use of iminium ion and α-amino radical intermediates, the elusive cyclic enamine intermediates were effectively generated by photoredox catalysis under mild conditions and efficiently captured by acetylene esters to form a wide array of bicyclic amino acid derivatives, thus enabling the simultaneous functionalization of two vicinal C(sp3)?H bonds.
- Xu, Guo-Qiang,Xu, Ji-Tao,Feng, Zhi-Tao,Liang, Hui,Wang, Zhu-Yin,Qin, Yong,Xu, Peng-Fei
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supporting information
p. 5110 - 5114
(2018/03/27)
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- Fused tricyclic hepatitis virus inhibitor and application thereof
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The invention belongs to the field of medical chemistry, relates to a fused tricyclic hepatitis virus inhibitor and application thereof, and particularly, provides a compound of the general formula I or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and a medicine composition containing the compounds and application of the compounds or the composition in medicine preparation. The compound has the good inhibiting activity on hepatitis C virus, meanwhile has the low toxicity on host cells, and is high in effectiveness, good in safety and likely to become the medicine for treating and/or preventing diseases relevant to HCV infection.
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Paragraph 0635; 0636; 0637; 0638
(2016/12/26)
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- Development of second generation gold-supported palladium material with low-leaching and recyclable characteristics in aromatic amination
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An improved process for the preparation of sulfur-modified gold-supported palladium material [SAPd, second generation] is presented. The developed preparation method is safer and generates less heat (aqueous Na 2S2O8 and H2SO4) for sulfur fixation on a gold surface, and it is superior to the previous method of preparing SAPd (first generation), which requires the use of the more heat-generating and dangerous piranha solution (concentrated H 2SO4 and 35% H2O2) in the sulfur fixation step. This safer and improved preparation method is particularly important for the mass production of SAPd (second generation) for which the catalytic activity was examined in ligand-free Buchwald-Hartwig cross-coupling reactions. The catalytic activities were the same between the first and second generation SAPds in aromatic aminations, but the lower palladium leaching properties and safer preparative method of second generation SAPd are a significant improvement over the first generation SAPd.
- Al-Amin, Mohammad,Arai, Satoshi,Hoshiya, Naoyoki,Honma, Tetsuo,Tamenori, Yusuke,Sato, Takatoshi,Yokoyama, Mami,Ishii, Akira,Takeuchi, Masashi,Maruko, Tomohiro,Shuto, Satoshi,Arisawa, Mitsuhiro
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p. 7575 - 7581
(2013/09/02)
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- COMPOUNDS AND METHODS
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Disclosed are compounds having formula I, wherein X1, X2, X3, R1, R2, R3, R4, R5, Y, A, Z, L, m and n are as defined herein, and methods of making and using the same.
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Page/Page column 60; 61; 63
(2013/03/26)
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- Ligand-free Buchwald-Hartwig aromatic aminations of aryl halides catalyzed by low-leaching and highly recyclable sulfur-modified gold-supported palladium material
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A stable heterogeneous catalyst precursor, sulfur-modified gold-supported palladium material (SAPd), has proved to be an excellent source of leached, ligand-free, Pd for the amination of aryl bromides and chlorides. The reaction-enabling catalyst is provided in situ as leached Pd in low catalyst loading (0.21±0.02mol%). This allows the precatalyst (SAPd) to be filtered off and used for a minimum of ten reaction cycles without loss of catalytic activity. SAPd released only trace amounts, less than 0.6ppm, of highly active Pd during the reaction without any aggregation. Copyright
- Al-Amin, Mohammad,Honma, Tetsuo,Hoshiya, Naoyuki,Shuto, Satoshi,Arisawa, Mitsuhiro
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supporting information; experimental part
p. 1061 - 1068
(2012/06/18)
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- 5-HYDROXYPYRIMIDINE-4-CARBOXAMIDE COMPOUND
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The present invention provides compounds which promote erythropoietin production. Compounds represented by the following general formula (1) or pharmacologically acceptable salts thereof are provided: [wherein, R1 represents a group —X-Q1, X-Q1-Y-Q2 or X-Q1-Y-Q2-Z-Q3, X represents a single bond, —CH2— or the like, Q1 represents a monocyclic or bicyclic heterocyclic group which may have substituent(s), Y represents a single bond, —CH2—, or the like, Q2 represents a monocyclic or bicyclic hydrocarbon ring group which may have substituent(s) or a monocyclic or bicyclic heterocyclic group which may have substituent(s), Z represents a single bond, —CR11R12— or the like, R11 and R12 each independently represents a hydrogen atom, a halogen atom or the like, Q3 represents a phenyl group which may have substituent(s), a C3-C7 cycloalkyl group which may have substituent(s), a C3-C7 cycloalkenyl group which may have substituent(s) or a monocyclic or bicyclic heterocyclic group which may have substituent(s), R2 represents a C1-C3 alkyl group or the like, and R3 represents a hydrogen atom or a methyl group].
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Page/Page column 23
(2011/05/16)
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- THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS
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The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer
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Page/Page column 257
(2010/09/18)
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- PIPERIDIN-4-YLPIPERAZINE COMPOUNDS FOR THE TREATMENT OF HCV INFECTION
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The invention relates to new piperazine-pieridine compounds having anti-viral activity and particularly anti-HCV activity. The invention further relates to pharmaceutical compositions comprising compounds according to the invention.
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Page/Page column 15
(2010/08/08)
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- An improved synthesis of N-aryl and N-heteroaryl substituted piperidones
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An efficient Pd(0)-catalyzed protocol for the rapid and efficient preparation of N-aryl and N-heteroaryl substituted piperidones is described. The two step syntheses proceed with an overall yield of 50-70% using X-Phos as optimal ligand for the Pd(0)-cata
- Sch?n, Uwe,Messinger, Josef,Buckendahl,Prabhu,Konda
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p. 2519 - 2525
(2008/02/02)
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- Total synthesis of (±)-pumiliotoxin C: An electrochemical approach
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The total stereoselective synthesis of the decahydroquinoline alkaloid (±)-pumiliotoxin C (cis-195A, 1) is described. The compound was prepared in 15 steps from the commercially available 4-piperidone ethylene ketal 2, in an overall 5% yield. New C-C bond
- Girard, Nicolas,Hurvois, Jean-Pierre,Moinet, Claude,Toupet, Loic
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p. 2269 - 2280
(2007/10/03)
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- Ligand- and Base-Free Copper(II)-Catalyzed C-N Bond Formation: Cross-Coupling Reactions of Organoboron Compounds with Aliphatic Amines and Anilines
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(Equation presented) A ligandless and base-free Cu-catalyzed protocol for the cross-coupling of arylboronic acids and potassium aryltrifluoroborate salts with primary and secondary aliphatic amines and anilines is described. The process utilizes catalytic copper(II) acetate monohydrate and 4 A molecular sieves in dichloromethane at slightly elevated temperatures under an atmosphere of oxygen. A broad range of functional groups are tolerated on both of the cross-coupling partners.
- Quach, Tan D.,Batey, Robert A.
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p. 4397 - 4400
(2007/10/03)
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- INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras
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