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The synthesis, crystal structure, and biological activity of new bis-cyclometalated compounds [M(ptpy)2(4-chloro-2-methyl-1,8-naphthyridine)]PF6[M = Rh (1); M = Ir (2); ptpy = 2-(p-tolyl)pyridinato] and [M(ptpy)2(2-methyl-1,8-naphthyridine)]PF6[M = Rh (3); M = Ir (4)] are described. The new compounds were prepared by the reaction of [{M(mu-Cl)(ptpy)2}2] (M = Rh, Ir) with the corresponding naphthyridine ligands. The molecular structures of compounds 1, 3, and 4 were confirmed by single-crystal X-ray diffraction studies.

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Yantai University; Zhu Yanping; Xie Rongji; Shao Tianqi; Song Liqun; Liu Kaixuan; Zhang Qiuyi; Yang Yijie; Sun Yuanyuan

The invention discloses a preparation method, of pyridopyrimidine and pyridopyrazole derivatives, which comprises: steps of preparing the substituted methylquinoline derivative, 6 – amino – 1111, 3-dimethylpyrimidine – 22224-diketone or 3 – methyl – 1 1-phenyl – 5 5-aminopyrazole and an iodine simple substance in a short, yield to industrially prepare such a compound as well as a derivative . and a preparation method 97%, of the method, and a preparation method, of. the, compound. (by machine translation)

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Within the wide range of nitrogen-containing heterocyclic compounds, the derivatives of 1,8-naphthyridine (NPTR) have gained a rising interest due to their reported versatile biological activities. The derivatives of NPTR scaffold are found to invite special interest from researchers nowadays on the significance of their manifestations of multiple attractive pharmacological activities which establish them as an effective and versatile tool in pharmaceutical chemistry and drug discovery. The diverse biological activities mainly include anti-inflammatory, antimicrobial, antiviral, anticancer, antihypertensive and analgesic activities. Novel NPTR scaffold has emerged its potency to treat neurological diseases like depression and Alzheimer’s disease. Further these agents possess different inhibitory activities, such as anti-HIV, anti-osteoporotic, alphavbeta3 antagonism, antimalarial, platelet aggregation, anti-oxidant, anti-allergic, gastric antisecretory, anticonvulsant, epidermal growth factor receptor (EGFR) inhibition, protein kinase inhibition, ionotropic properties, beta3 antagonism, phosphodiesterase 4 (PDE 4) inhibitions, adenosine receptor agonistic activity, adrenoceptors antagonism and DNA stabilizing activity, etc. In this review, we highlight the updates of different 1,8-naphthyridine derivatives and explain the key data available in the context of various biological activities of NPTR derivatives available from the literature. This may direct opportunity in researches in the synthesis of novel medicinal agents and the development of new heterocycles for modification of existing biological actions as well as evaluation of other possible pharmacological activities.

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SmithKline Beecham Corporation

A compound of the formula (I) is disclosed which is a vitronectin receptor antagonist and is useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 1569-16-0, name is 2-Methyl[1,8]-Naphthyridine, introducing its new discovery. Recommanded Product: 2-Methyl[1,8]-Naphthyridine

A new aerobic copper-catalyzed halocyclization reaction of methyl N-heteroaromatics and aliphatic amines has been developed, which enables straightforward access to functionalized imidazo-fused N-heterocycles with the merits of good functional tolerance, use of easily available copper salts as the catalysts, lithium halides as the halogen sources, and O2 as a sole oxidant. Due to the reaction features’ selective introduction of halogen functionalities to the newly formed imidazo ring, further extensions of the developed chemistry toward synthetic diversity, including effective access to functional materials, are easily envisioned.

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Two new palladium (II) complexes containing a 1,10-phenanthroline analogue N-heterocyclic carbene (NHC) have been synthesized. The complexes were characterized by 1H and 13C NMR spectroscopy and elemental analysis and their structures were determined by single-crystal X-ray diffraction. The NHC-palladium complexes were employed as catalysts for Suzuki-Miyaura coupling reactions of aryl chlorides with arylboronic acids in aqueous media at room temperature. The cross-coupling reactions were highly efficient with low catalysts loadings.

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A straightforward method for the palladium-catalyzed triarylation of heteroarylmethanes at the methyl group has been developed. The reaction works with a variety of aryl halides, enabling the rapid synthesis of triaryl(heteroaryl)methanes in moderate to excellent yields. (Figure presented.).

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Carbanions of alpha-haloalkyl aryl sulfones, sulfonates, and sulfonamides react with bicyclic heteroaromatic compounds (quinoxalines, naphthyridines, and 5-azaquinoxalines) according to two general pathways: vicarious nucleophilic substitution of hydrogen and/or bisannulation.In some cases other competitive reactions such as SNAr are observed.Factors governing the direction of these reactions are discussed in terms of the charge distribution in the anionic ? adducts and the reaction conditions.

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A copper-catalyzed transfer aldol type reaction of beta-hydroxy ketones or nitriles with aldehydes is reported, which enables chemo- and stereoselective access to (E)-alpha,beta-unsaturated ketones and (E)-acrylonitriles. A key step of the in situ copper(i)-promoted retro-aldol reaction of beta-hydroxy ketones or nitriles is proposed to generate a reactive Cu(i) enolate or cyanomethyl intermediate, which undergoes ensuing aldol condensation with aldehydes to deliver the products. This reaction uses 1.2 mol% Cu(IPr)Cl (IPr denotes 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene) as the catalyst in the presence of 6.0 mol% NaOtBu cocatalyst at room temperature or 70 C. A range of aryl and heteroaryl aldehydes as well as acrylaldehydes are compatible with many useful functional groups being tolerated. Under the mild and weakly basic conditions, competitive Cannizzaro-type reaction of benzaldehydes and side reactions of base-sensitive functional groups can be effectively suppressed, which show synthetic advantages of this reaction compared to classic aldol reactions. The synthetic potential of this reaction is further demonstrated by the one-step synthesis of biologically active quinolines and 1,8-naphthyridine in excellent yields (up to 91%). Finally, a full catalytic cycle for this reaction has been constructed using DFT computational studies in the context of a retro-aldol/aldol two-stage mechanism. A rather flat reaction energy profile is found indicating that both stages are kinetically facile, which is consistent with the mild reaction conditions.

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Oxazoline and camphor-pyrazole units are introduced on the 1,8-naphthyridine scaffold to access chiral ligands L1, L2 and L3. Metalation of these chiral ligands with Cu(I) and Ag(I) precursors afforded di- and tetranuclear complexes [Cu4I4(L1)2] (1), [Cu4I4(L2)2] (2), [Cu2I2(L3)] (3), [Cu2I(L2)2](OTf) (4), [Ag2(L1)2](OTf)2 (5) and [Ag4(L2)4Br](OTf)3 (6), containing [M4Xn] (n = 1,4 and X = Br, I) or [M2Xn] (n = 0, 1, 2 and X = I) core. All complexes are structurally characterized. Naphthyridine-derived ligands reveal bridge-chelate coordination motif and hold two metal centers in close proximity. The tetranuclear complexes are dimer of dinuclear complexes bridged by the halides. Electronic absorption and emission spectra of copper complexes are reported. Catalytic utility of all complexes are examined for asymmetric transformations but they showed poor activity probably due to limited solubility and coordinative saturation at the metal centers. The best results are obtained with [L3/Cu salt] combination for cyclopropanation of styrene, N?H bond insertion and nitroaldol (Henry) reactions with very low enantioselectivity.

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