- Recyclable covalent triazine framework-supported iridium catalyst for the N-methylation of amines with methanol in the presence of carbonate
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An iridium complex Cp*Ir@CTF, which is synthesized by the coordinative immobilization of [Cp*IrCl2]2 on a functionalized covalent triazine framework (CTF), was found to be a general and highly efficient catalyst for the N-methylation of amines with methanol in the presence of carbonate. Under environmentally benign conditions, a variety of desirable products were obtained in high yields with complete selectivities and functional group friendliness. Furthermore, the synthesized catalyst could be recycled by simple filtration without obvious loss of catalytic activity after sixth cycle. Notably, this research exhibited the potential of covalent triazine framework-supported transition metal catalysts for hydrogen autotransfer process.
- Liu, Peng,Yang, Jiazhi,Ai, Yao,Hao, Shushu,Chen, Xiaozhong,Li, Feng
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p. 281 - 290
(2021/03/26)
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- N-Methylation of Amines with Methanol Catalyzed by a Cp?Ir Complex Bearing a Functional 2,2′-Bibenzimidazole Ligand
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A new type of Cp?Ir complex bearing a functional 2,2′-bibenzimidazole ligand was designed, synthesized, and found to be a highly effective and general catalyst for the N-methylation of a variety of amines with methanol in the presence of a weak base (0.3 equiv of Cs2CO3).
- Liang, Ran,Li, Shun,Wang, Rongzhou,Lu, Lei,Li, Feng
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supporting information
p. 5790 - 5793
(2017/11/10)
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- General and efficient method for direct N-monomethylation of aromatic primary amines with methanol
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The direct N-monomethylation of aromatic primary amines, including arylamines, arylsulfonamides and amino-azoles, using methanol as a methylating agent has been accomplished in the presence of a [CpIrCl2]2/NaOH system. From both synthetic and environmental points of view, the reaction is highly attractive because of low catalyst loading, broad substrate scope and excellent selectivities.
- Li, Feng,Xie, Jianjiang,Shan, Haixia,Sun, Chunlou,Chen, Lin
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p. 8645 - 8652
(2015/03/05)
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- Synthesis and cytotoxicity studies of quinoline-3-carbonitrile derivatives
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A series of quinoline-3-carbonitrile derivatives were designed and synthesized. Their cytotoxicity in vitro against four cancer cell lines (A549, HT-29, MDA-MB-231 and SMMC-7721) were evaluated by standard MTT assay. The pharmacological results showed that most of the prepared compounds displayed excellent selective cytotoxicity toward SMMC-7721 cell line. Among them, compounds 7c, 7e, 11b, 11f and 11g were more active than Gefitinb against SMMC-7721 cell line.
- Zhang, Shu Lan,Zhai, Xin,Zhang, Shi Jiao,Yu, Hong Hao,Gong, Ping
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scheme or table
p. 939 - 942
(2011/11/13)
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- GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
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GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
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Page/Page column 103
(2008/12/04)
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- Direct, catalytic hydroaminoalkylation of unactivated olefins with N-alkyl arylamines
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A tantalum-catalyzed addition of N-alkyl arylamine ∞-C-H bonds across olefins is reported. These reactions occur with mono- and 2,2-disubstituted olefins to form the branched insertion products in high yield and regioselectivity. The reactions encompass additions of the ∞-C-H bonds of cyclic and acyclic amines, as well as intramolecular additions. NMR studies indicate that the starting homoleptic, Ta(NMe2)5 precatalyst converts to bis- and tris(N-methylanilide) complexes (among others) in solution. Deuterium-labeling studies suggest that reversible ortho-metalation of the arene substituent occurs under the reaction conditions. However, several experiments imply that this ortho-metalation does not lie on the reaction pathway. Instead, these complexes are proposed to eliminate amine to form N-aryl imine complexes, which insert olefins into the Ta-C bond and undergo protonolysis to regenerate the active catalyst and eliminate the addition product. Copyright
- Herzon, Seth B.,Hartwig, John F.
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p. 6690 - 6691
(2008/02/06)
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- Prodrugs of neuron-selective monoamine oxidase inhibitors: Amino acid derivatives of 1-(4-aminophenyl)-2-aminopropanes
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Six amino acid derivatives of 1-(4-aminophenyl)-2-aminopropanes and their parent amines were synthezised and tested for their potency and selectivity in inhibiting monoamine oxidase (MAO) in vitro and in vivo. The amino acid derivatives were 300-1000 times less potent than the parent amines in inhibiting the MAO-A activity in a rat brain mitochondrial preparation in vitro. All compounds, except the (R)-valinamide derivative (22), were potent inhibitors of MAO in the rat brain in vivo and were, like the parent amines markedly more potent within the monoaminergic neurons than in other neurons. The glycinamide derivative 7 showed the largest difference between intra- and extra-neuronal inhibition in serotonergic neurons. The time course of the inhibitory effect of 7 in vivo showed that it is a reversible inhibitor with a long duration.
- Florvall, Lennart,Fagervall, Ingrid,Larsson, Lars-Gunnar,Ross, Svante B.
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p. 137 - 151
(2007/10/03)
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