cas 30483-75-1, N-(4-BROMOPHENYL)MORPHOLINE

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The surprisingly facile formation of Pd(i)-phosphido complexes from: Ortho -biphenylphosphines and palladium acetate
The widely-used ortho-biphenylphosphine ligands SPhos and RuPhos not only undergo facile orthometallation with palladium acetate, yielding strained, four-membered dimeric palladacycles but more surprisingly, in the presence of alcoholic solvents, along with the less encumbered analogue MePhos, yield unusual dinuclear Pd(i) complexes, in which the Pd-centers are bridged by both a phosphide ligand and by the arene of a coordinated phosphine donor.
Montgomery, Michelle,O'Brien, Harry M.,Méndez-Gálvez, Carolina,Bromfield, Caitlin R.,Roberts, Jack P. M.,Winnicka, Anna M.,Horner, Andrew,Elorriaga, David,Sparkes, Hazel A.,Bedford, Robin B.
p. 3539 - 3542
(2019)
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Room-temperature phosphorescent material as well as preparation method and application thereof
The invention relates to the technical field of phosphorescent materials. The invention provides a room-temperature phosphorescent material and a preparation method and application thereof. As C-H.O. O, C-H. Experimental results show that the material pro
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Paragraph 0083-0086

(2021/09/21)

Amination of Aryl Halides Mediated by Electrogenerated Nickel from Sacrificial Anode
Electrochemical C(sp2)?N couplings mediated by nickel salts generated from the sacrificial anode has been described for the first time. In this approach, the sacrificial nickel anode is employed as the sole source of nickel and the process, operationally simple to set up, enables the preparation of functionalized arylamine derivatives with moderate to good yields, under mild reaction conditions and without additional ligand. A cooperative process between the two electrodes is involved in the proposed mechanism.
Daili, Farah,Sengmany, Stéphane,Léonel, Eric
p. 2462 - 2469
(2021/06/28)

Synthesis of some new distyrylbenzene derivatives using immobilized Pd on an NHC-functionalized MIL-101(Cr) catalyst: photophysical property evaluation, DFT and TD-DFT calculations
In this study the catalytic application of a heterogeneous Pd-catalyst system based on metal organic framework [Pd-NHC-MIL-101(Cr)] was investigated in the synthesis of distyrylbenzene derivatives using the Heck reaction. The Pd-NHC-MIL-101(Cr) catalyst s
Niknam, Esmaeil,Mahmoodi, Ali,Panahi, Farhad,Heydari Dokoohaki, Maryam,Zolghadr, Amin Reza,Khalafi-Nezhad, Ali
p. 12374 - 12380
(2021/04/07)

Direct bromodeboronation of arylboronic acids with CuBr2 in water
An efficient and practical method has been developed for the preparation of aryl bromides via the direct bromodeboronation of arylboronic acids with CuBr2 in water. This strategy provides several advantages, such as being ligand-free, base-free, high yielding, and functional group tolerant.
Tang, Yan-Ling,Xia, Xian-Song,Gao, Jin-Chun,Li, Min-Xin,Mao, Ze-Wei
supporting information

(2021/01/05)

Effect of Precatalyst Oxidation State in C-N Cross-Couplings with 2-Phosphinoimidazole-Derived Bimetallic Pd(I) and Pd(II) Complexes
We report the catalytic activity of two phosphinoimidazole-derived bimetallic palladium complexes in Pd-catalyzed amination reactions. Our studies demonstrate that the starting oxidation state (Pd(I) or Pd(II)) of the dimeric complex has a significant effect on the efficiency of the catalytic reaction. The corresponding Pd(I) complex shows higher reactivity in Buchwald-Hartwig aminations, while the Pd(II) complex is much more reactive in carbonylative amination reactions. These new dimeric palladium complexes provide good to excellent reactivity and yields in the amination reactions tested.
Martinez, Erin E.,Moreno, Mariur Rodriguez,Barksdale, Caleb A.,Michaelis, David J.
supporting information
p. 2763 - 2767
(2021/08/27)

Visible light-induced mono-bromination of arenes with BrCCl3
A highly efficient and regioselective bromination of electron-rich arenes and heteroarenes using commercially available BrCCl3as a “Br” source has been developed. The reaction was performed in air under mild conditions with photocatalyst Ru(bpy)3Cl2·6H2O, avoiding the usage of strong acids and strong oxidants. Mono-brominated products were obtained with medium to excellent yields (up to 94%). This strategy has shown good compatibility and highpara-selectivity, which will facilitate the complicated synthesis.
Fan, Jiali,Wei, Qiancheng,Zhu, Ershu,Gao, Jing,Cheng, Xiamin,Lu, Yongna,Loh, Teck-Peng
supporting information
p. 5977 - 5980
(2021/06/18)

COMPOUND SIMULTANEOUSLY INHIBITING LSD1 AND HDAC TARGETS AND APPLICATION THEREOF
A compound having a general structural formula as shown in Formula I: X-AB-Y (Formula I); in the above Formula I, X is selected from any one of -CO2H, -CONHZ, -CH=CH-CO2H, -CH=CH-CONHZ, wherein Z is selected from any one of substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted aryl, and hydroxyl; Y = -NR1R2, wherein NR1R2 is a substituted or unsubstituted 3- to 9-membered nitrogen-containing heterocycloalkyl; A and B are each independently selected from substituted or unsubstituted phenylene, substituted or unsubstituted azaphenylene. The compound or corresponding pharmaceutical salt thereof can inhibit LSD1 and HDAC target proteins at the same time, thus inhibit the proliferation of many kinds of tumor cells and have good antitumor effect.
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Paragraph 0041; 0047-0048; 0052

(2020/11/26)

NOVEL APOPTOSIS SIGNAL-REGULATING KINASE 1 INHIBITORS
The present invention relates to inhibitors of apoptosis signal-regulating kinase 1 ("ASK1"), a process for synthesis of the compounds of the present invention, composition comprising the compounds and use of the compounds for inhibition of ASK1.
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(2021/01/23)

Catalyst-free photodecarbonylation ofortho-amino benzaldehyde
It is almost a consensus that decarbonylation of the aldehyde group (-CHO) needs to not only be mediated by transition metal catalysts, but also requires severe reaction conditions (high temperature and long reaction time). In this work, inspired by the “conformational-selectivity-based” design strategy, we broke this consensus and discovered a catalyst-free photodecarbonylation of the aldehyde group. It revealed that decarbonylation can be easily achieved with visible light irradiation by introducing a tertiary amine into theortho-position of the aldehyde group. A diverse array of tertiary amines is tolerated by our photodecarbonylation under mild conditions. Furthermore, the (QM) computations of the mechanism and the experiments on well-designed special substrates revealed that our photodecarbonylation depends on the conformational specificity of the aldehyde group and tertiary amine, and occurs through an unusual [1,4]-H shift and a subsequent [1,3]-H shift.
Li, Lamei,Wang, Songping,Wei, Wentao,Yan, Ming,Zhou, Jingwei
supporting information
p. 3421 - 3426
(2020/06/25)

Aryl halide and synthesis method and application thereof
The invention discloses a synthesis method of aryl halides (including aryl bromide shown as a formula (2) and aryl iodide shown as a formula (3)). All the systems are carried out in an air atmosphere,visible light is utilized to excite a substrate or a photosensitizer to catalyze the reaction; and in a reaction solvent, when aromatic hydrocarbon shown in the formula (1) and sodium bromide serve as raw materials, aryl bromide shown in the formula (2) is obtained through a reaction under the auxiliary action of an additive (protonic acid); or when aromatic hydrocarbon shown in the formula (1) and sodium iodide are used as raw materials, under the auxiliary action of an additive (protonic acid), aryl iodide shown in the formula (3) is obtained through reaction. The synthesis method has the advantages of cheap and accessible raw materials, simple reaction operation and mild reaction conditions. The method is compatible with the arylamine which is liable to be oxidized. The invention provides a new method for the synthesis of aryl halides, realizes the amplification of basic chemicals aryl halides including aryl bromide shown in the formula (2) and aryl iodide shown in the formula (3),and has wide application prospect and practical value.
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Paragraph 0094-0096

(2020/06/02)

Visible-light-promoted oxidative halogenation of (hetero)arenes
Organic halides are critical building blocks that participate in various cross-coupling reactions. Furthermore, they widely exist as natural products and artificial molecules in drugs with important physiological activities. Although halogenation has been well studied, to the best of our knowledge, studies focussing on sensitive systems (e.g.aryl amines) have not been reported. Herein, we describe a compatible oxidative halogenation of (hetero)arenes with air as the oxidant and halide ions as halide sources under ambient conditions (visible light, air, aqueous system, room temperature, and normal pressure). Moreover, this protocol is practically feasible for gram-scale synthesis, showing potential for industrial application.
Jiang, Xuefeng,Li, Yiming,Lu, Lingling
supporting information
p. 5989 - 5994
(2020/10/18)

Photo-induced dealdehyding method
The invention provides a photo-induced dealdehyding method, and belongs to the technical field of organic synthesis. The photo-induced dealdehyding method comprises the following steps that a mixtureof a compound shown in the formula I and a solvent are reacted under an inert gas atmosphere and visible light irradiation, a dealdehyding product is obtained, and no photocatalyst is used in the whole process; wherein the structural formula of the formula I shown in the specification, R is a functional group and is selected from hydrogen, methyl, methoxyl, cyano, chlorine, bromine or fluorine. According to the photo-induced dealdehyding method, in the inert gas atmosphere, the compound shown in the formula (I) can be excited to generate carbon-oxygen bond homogeneous cracking through visiblelight irradiation, then free radical migration and double bond displacement are conducted, finally carbon monoxide is removed, aldehyde group removal is completed, no photocatalyst is needed in the whole process, operation is easy and convenient, and conditions are mild.
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Paragraph 0048-0053; 0066-0071

(2020/06/16)

Palladium nanoparticles supported on cysteine-functionalized MNPs as robust recyclable catalysts for fast O- and N-arylation reactions in green media
A magnetically robust recyclable nanocatalyst was fabricated by immobilizing of Pd onto the surface of cysteine-functionalized magnetic nanoparticles (MNPs?Cys-Pd). This nanocatalyst was characterized using various techniques such as FT-IR, XRD, TEM, SEM, EDX, VSM, and ICP. The application of catalyst (MNPs?Cys-Pd) was investigated for O-arylation and N-arylation reactions. This phosphine-free complex was found as highly efficient heterogeneous catalyst in green media and mild reaction conditions. In addition, it gave excellent recyclability without significant deactivation after ten cycles.
Hajipour, Abdol R.,Khorsandi, Zahra,Fatemeh Mohammadi Metkazini
(2019/08/12)

Electrochemical Regioselective Bromination of Electron-Rich Aromatic Rings Using n Bu 4 NBr
Electrochemical regioselective bromination of electron-rich aromatic rings using stoichiometric tetrabutylammonium bromide (n Bu 4 NBr) has been accomplished under mild conditions. This protocol provides an environmentally friendly and simple way for the construction of C-Br bond in moderate to high yields with wide functional group tolerance.
Bai, Ya,Che, Xin,Liu, Nian,Ning, Shulin,Shi, Lingling,Wang, Shutao,Wang, Siyu,Xiang, Jinbao,Xie, Wenxia
p. 1313 - 1316
(2019/06/20)

Cu-mediated selective bromination of aniline derivatives and preliminary mechanism study
A simple and efficient bromination of aniline, aniline derivatives, and analogs have been developed. Forty three examples were given and the highest yield reached was 98%. Different substrates including substituted aniline, pyridin-amine, N-substituted aniline, N,N-disubstituted aniline, N-phenyl-amide, N-phenyl-sulfonamide, and nitrogen-containing heterocycles were all reactive and selectively generated desired bromo-products. The method can be applied to synthesize drug intermediate and quinoxaline derivatives.
Zhao, Hong-Yi,Yang, Xue-Yan,Lei, Hao,Xin, Minhang,Zhang, San-Qi
supporting information
p. 1406 - 1415
(2019/05/01)

Synthesis of novel triazine compound and application thereof as luminescent material
The invention relates to a synthesis of a novel triazine compound and an application thereof as a luminescent material. The structural formula of the novel triazine compound is shown in (I). (Shown inthe description) Ar is selected from aryl, substituted aryl and aryl containing heteroatoms; and R1 is selected from chlorine atom, trifluoromethyl and butoxy.
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Paragraph 0052; 0054

(2019/04/17)

CATHEPSIN K INHIBITOR AND APPLICATION THEREOF
The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.
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Paragraph 0306

(2018/07/29)

Pharmacomodulation on Gold-NHC complexes for anticancer applications – is lipophilicity the key point?
A series of four new mononuclear cationic gold(I) complexes containing nitrogen functionalized N-heterocyclic carbenes (NHCs) was synthesized and fully characterized by spectroscopic methods. The X-ray structures of three complexes are presented. These lipophilic gold(I) complexes originate from a pharmacomodulation of previously described gold(I)-NHC complexes, by replacing an aliphatic spacer with an aromatic one. The Log P values of the resulting complexes increased by 0.7–1.5, depending on the substituents in comparison to the aliphatic-linker systems. The new series of complexes has been investigated in vitro for their anti-cancer activities in PC-3 (prostate cancer) and T24 (bladder cancer) cell lines and in the non-cancerous MC3T3 (osteoblast) cell line. All tested complexes show high activities against the cancer cell lines with GI50 values lower than 500 nM. One complex (11) has been selected for further investigations. It has been tested in vitro in six cancer cell lines from different origins (prostate, bladder, lung, bone, liver and breast) and two non-cancerous cell lines (osteoblasts, fibroblasts). Moreover, cellular uptake measurements were indicative of a good bioavailability. By various biochemical assays, this complex was found to effectively inhibit the thioredoxin reductase (TrxR) and its cytotoxicity towards prostate PC-3, bladder T24 and liver HepG2 cells was found to be ROS-dependent.
Zhang, Chen,Maddelein, Marie-Lise,Wai-Yin Sun, Raymond,Gornitzka, Heinz,Cuvillier, Olivier,Hemmert, Catherine
p. 320 - 332
(2018/08/17)

Making Copper(0) Nanoparticles in Glycerol: A Straightforward Synthesis for a Multipurpose Catalyst
Small zero-valent copper nanoparticles (CuNPs) have been straightforwardly prepared from Cu(I) and Cu(II) precursors in glycerol and in the presence of polyvinylpyrrolidone as stabilizer. Thanks to the negligible vapor pressure of the solvent, these original nano-systems could be directly characterized in glycerol as well as in the solid state, exhibiting relevantly homogeneous colloidal dispersions, also even after catalysis. CuNPs coming from the well-defined coordination complex di-μ-hydroxobis[(N,N,N′,N′-tetramethylethylenediamine)copper(II)] chloride {[Cu(κ2-N,N-TMEDA)(μ-OH)]2Cl2} have been highly efficient in C–C and C–heteroatom bond formation processes. This new catalytic system has proved its performance in C–N couplings and in the synthesis of differently substituted propargylic amines through cross-dehydrogenative couplings, multi-component reactions such as A3 (aldehyde-alkyne-amine) and KA2 (ketone-alkyne-amine) couplings, as well as in the formation of heterocycles such as benzofurans, indolizines, and quinolines under smooth conditions. No significant copper amount was detected in the extracted organic compounds from the catalytic phase by inductively coupled plasma-atomic emission spectroscopic (ICP-AES) analyses, proving a highly efficient immobilization of copper nanoparticles in glycerol. From a mechanistic point of view, spectroscopic data (infrared and ultraviolet-visible spectra) agree with a surface-like catalytic reactivity. (Figure presented.).
Dang-Bao, Trung,Pradel, Christian,Favier, Isabelle,Gómez, Montserrat
p. 2832 - 2846
(2017/08/23)

Zwitterionic-Salt-Catalyzed Site-Selective Monobromination of Arenes
A zwitterionic-salt-catalyzed electrophilic monobromination of arenes with high regioselectivity has been developed. Under mild reaction conditions, a wide range of monobrominated aromatic compounds can be obtained in excellent yields. The reaction can be operated using an extremely low catalyst loading (0.05 mol %) with the inexpensive brominating agent N-bromosuccinimide. The versatility of this catalytic protocol has been demonstrated by the scale-up reaction with a 0.01 mol % catalyst loading to provide the selectively halogenated compound in quantitative yield.
Xiong, Xiaodong,Tan, Fei,Yeung, Ying-Yeung
supporting information
p. 4243 - 4246
(2017/08/23)

Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs
Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).
Beinat, Corinne,Reekie, Tristan,Banister, Samuel D.,O'Brien-Brown, James,Xie, Teresa,Olson, Thao T.,Xiao, Yingxian,Harvey, Andrew,O'Connor, Susan,Coles, Carolyn,Grishin, Anton,Kolesik, Peter,Tsanaktsidis, John,Kassiou, Michael
supporting information
p. 277 - 301
(2015/03/31)

Efficient and Practical Oxidative Bromination and Iodination of Arenes and Heteroarenes with DMSO and Hydrogen Halide: A Mild Protocol for Late-Stage Functionalization
An efficient and practical system for inexpensive bromination and iodination of arenes as well as heteroarenes by using readily available dimethyl sulfoxide (DMSO) and HX (X = Br, I) reagents is reported. This mild oxidative system demonstrates a versatile protocol for the synthesis of aryl halides. HX (X = Br, I) are employed as halogenating reagents when combined with DMSO which participates in the present chemistry as a mild and inexpensive oxidant. This oxidative system is amenable to late-stage bromination of natural products. The kilogram-scale experiment (>95% yield) shows great potential for industrial application.
Song, Song,Sun, Xiang,Li, Xinwei,Yuan, Yizhi,Jiao, Ning
supporting information
p. 2886 - 2889
(2015/06/30)

SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 132; 133

(2015/01/07)

Selective bromination of pyrrole derivatives, carbazole and aromatic amines with DMSO/HBr under mild conditions
Bromination of pyrrole derivatives, carbazole and aromatic amines using the DMSO/HBr system affords high yields of the corresponding bromo compounds. Temperature control used in the bromination of anilines helped to promote selective formation of mono- or di-brominated products. Simple operation, low toxicity and high selectivity make this a promising new procedure for the bromination of aromatic compounds.
Liu, Cong,Dai, Rongji,Yao, Guowei,Deng, Yulin
p. 593 - 596
(2015/01/09)

Copper-catalyzed electrophilic amination of arylsilanes with hydroxylamines
A copper-catalyzed electrophilic amination of aryl[(2-hydroxymethyl)phenyl] dimethylsilanes with O-acylated hydroxylamines has been developed to afford the corresponding anilines in good yields. The catalytic reaction proceeds very smoothly under mild conditions and tolerates a wide range of functional groups.
Miki, Yuya,Hirano, Koji,Satoh, Tetsuya,Miura, Masahiro
supporting information
p. 172 - 175
(2013/03/28)

Transition-metal-free electrophilic amination of arylboroxines
A transition-metal-free strategy to construct C(sp2)-N bonds using arylboroxines and O-benzoyl hydroxylamines as coupling partners has been developed. This transformation provides a useful method to access various aromatic amines.
Xiao, Qing,Tian, Leiming,Tan, Renchang,Xia, Ying,Qiu, Di,Zhang, Yan,Wang, Jianbo
experimental part
p. 4230 - 4233
(2012/09/22)

Copper-catalyzed amination of arylboronates with N,N-dialkylhydroxylamines
A tolerant coupling: The title reaction has been developed to deliver arylamines (see scheme; Bz=benzoyl, dppbz=1,2-bis(diphenylphosphino)benzene). The catalysis is based on electrophilic, umpolung amination and enables the use of secondary acyclic amines. Various functional groups are tolerated, thus opening up a new substrate class for the Chan-Lam-type coupling.
Matsuda, Naoki,Hirano, Koji,Satoh, Tetsuya,Miura, Masahiro
p. 3642 - 3645
(2012/05/20)

Synthesis of hindered anilines: Copper-catalyzed electrophilic amination of aryl boronic esters
No longer a hindrance: Copper-catalyzed electrophilic amination of aryl boronic esters is accomplished under mild reaction conditions using 2.5-5.0 mol % of a catalyst derived from copper tert-butoxide and Xantphos ligand (see scheme). The reaction tolerates a wide range of functional groups and can be used to prepare some of the most hindered anilines made to date. Copyright
Rucker, Richard P.,Whittaker, Aaron M.,Dang, Hester,Lalic, Gojko
supporting information; experimental part
p. 3953 - 3956
(2012/06/04)

A Green protocol for the bromination and iodination of the aromatic compounds using H5IO6/NaBr and H5IO 6/NaI in the water
Bromination and iodination of the aromatic compounds have efficiently been carried out at room temperature and 70 °C, respectively, in short reaction times using orthoperiodic acid/sodium bromide (1:2) and orthoperiodic acid/sodium iodide (1:2) in water to prepare the corresponding halo compounds with excellent yields.
Yousefi-Seyf, Jaber,Tajeian, Kazem,Kolvari, Eskandar,Koukabi, Nadiya,Khazaei, Ardeshir,Zolfigol, Mohammad Ali
p. 2619 - 2622
(2012/10/29)

Imidazolium-containing diselenides for catalytic oxidations with hydrogen peroxide and sodium bromide in aqueous solutions
The design and synthesis of imidazolium-containing diselenides 4a-c is described. The introduction of the N-methylimidazolium group gives freely soluble compounds in water, unlike the majority of common organic diselenides. Catalytic amounts of 4a-c effectively promote bromination of organic substrates using a safe and inexpensive NaBr/H2O2 system in water. Kinetics experiments revealed that the bromination of 4-pentenoic acid has a first-order dependence with respect to both NaBr and H2O2 concentrations The rate of reaction was also sensitive to the pH of the solution. Preparative reactions showed that, compared to 4a, diphenyl diselenide 5 was a poor catalyst and the ionic liquid 1-benzyl-3-methylimidazolium bromide 6 showed no catalytic activity with H2O2 indicating synergy from the combined functionality.
Alberto, Eduardo E.,Detty, Michael R.,Braga, Antonio L.
p. 10476 - 10481,6
(2012/12/12)

Cu-catalyzed carbon-heteroatom coupling reactions under mild conditions promoted by resin-bound organic ionic bases
Resin-bound organic ionic bases (RBOIBs) were developed in which tetraalkyl-ammonium or phosphonium cations are covalently attached to solid resins. The application tests showed that the performance of the tetraalkyl-ammonium-type RBOIBs is slightly better than that of the corresponding Cs salts in Cu-catalyzed C-N cross-couplings, while the tetraalkylphosphonium-type RBOIBs are significantly better than all the inorganic bases. With these newly developed RBOIBs, room-temperature Cu-catalyzed C-Ncoupling with various nonactivated aryl iodides and even aryl bromides can be readily accomplished. Moreover, RBOIBs can be easily recycled and reused for a number of times without much drop of activity. The good performances of RBOIBs are proposed to arise from the relatively weak binding forces between the cationic polymer backbone and basic anions, as opposed to the strong metal-anion interactions in the inorganic bases. Further applications of RBOIBs in Ni-catalyzed Suzuki-type couplings at room temperature, Cu-catalyzed C-N couplings at -30 °C, a Pd-catalyzed Heck reaction at 60 °C, and Cu-catalyzed C-S couplings at room temperature demonstrate that RBOIBs are generally applicable bases with improved performance for many other types of organic transformations.
Huang, Yao-Bing,Yang, Chu-Ting,Yi, Jun,Deng, Xiao-Jian,Fu, Yao,Liu, Lei
experimental part
p. 800 - 810
(2011/04/22)

C-N bond formation catalysed by CuI Bonded to polyaniline nanofiber
Polyaniline nanofiber as a macroligand for the supported cuprous iodide catalyst (CuI-PANInf) has been developed for the coupling of aryl halides (including aryl chlorides) with aliphatic, aromatic, and N(H)-heterocyclic amines under ambient conditions (80 °C for aryl chlorides) has been developed. This simple and efficient method for coupling reactions is highly versatile, convenient, and also the catalyst can be used for several cycles with good-to-excellent yields.
Arundhathi, Racha,Kumar, Desitti Chaitanya,Sreedhar, Bojja
supporting information; experimental part
p. 3621 - 3630
(2010/08/20)

Electrophilic bromination of alkenes, alkynes, and aromatic amines with iodic acid/potassium bromide under mild conditions
Bromination of alkenes, alkynes, and aromatic amines has efficiently been carried out at room temperature in short reaction times using HIO 3/KBr in CH2Cl2/H2O (1:1) to prepare corresponding brominated compounds in excellent yields.
Khazaei, Ardeshir,Zolfigol, Mohammad Ali,Kolvari, Eskandar,Koukabi, Nadiya,Soltani, Hamid,Bayani, Leyla Sharaf
experimental part
p. 2954 - 2962
(2010/10/20)

Cu-Al hydrotalcite: An efficient and reusable ligand-free catalyst for the coupling of aryl chlorides with aliphatic, aromatic, and N(H)-heterocyclic amines
Copper-aluminum hydrotalcite catalysts were effectively used in the coupling of aryl chlorides with aliphatic, aromatic, and N(H)-heterocyclic amines to afford the corresponding N-alkylated/arylated amines in excellent yields. The catalyst was quantitatively recovered from the reaction by simple filtration and reused for a number of cycles with almost consistent activity. Georg Thieme Verlag Stuttgart.
Sreedhar,Arundhathi,Linga Reddy,Amarnath Reddy,Lakshmi Kantam
experimental part
p. 2517 - 2522
(2010/03/24)

Elctrophilic bromination of alkenes, alkynes, and aromatic amines with potassium bromide/orthoperiodic acid under mild conditions
Bromination of alkenes, alkynes, and aromatic amines has efficiently been carried out at room temperature in short reaction times using potassium bromide/orthoperiodic acid in dichloromethane-water (1:1) to prepare the corresponding bromo compounds with excellent yields.
Khazaei, Ardeshir,Zolfigol, Mohammad Ali,Kolvari, Eskandar,Koukabi, Nadiya,Soltani, Hamid,Komaki, Fatemeh
experimental part
p. 3672 - 3676
(2010/04/05)

Palladium-catalyzed monoamination of dihalogenated benzenes
The palladium-catalyzed monoamination of symmetric dibromobenzenes can be performed using a catalyst based on Pd2dba3 and BINAP in the presence of NaO(t-Bu). The analogous transformation of non-symmetric bromoiodobenzenes is most effectively performed with Xantphos as the ligand, while reactions with BINAP were non-selective. These transformations can be scaled uneventfully to >10 g quantities. They do not require drybox or Schlenk techniques, and all reagents are weighed out in air. The resulting monobromoanilines are versatile intermediates for further synthetic transformations.
Larsen, Simon Birks?,Bang-Andersen, Benny,Johansen, Tommy N?rskov,J?rgensen, Morten
p. 2938 - 2950
(2008/09/19)

A xerogel-sequestered selenoxide catalyst for brominations with hydrogen peroxide and sodium bromide in an aqueous environment
(Chemical Equation Presented) 4-(Hydroxymethyl)phenyl benzyl selenoxide (4) sequestered in a halide-permeable, Class II xerogel formed from 10/90 (mol/mol) 3-aminopropyltriethoxysilane/tetraethoxysilane catalyzes the bromination of organic substrates (4-pentenoic acid, 3,5-dihydroxybenzoic acid, 1,3,5-trimethoxybenzene, N-phenylmorpholine, and N,N-dimethylaniline) with NaBr and H2O2. Catalyst performance (reaction rate) when sequestered within the halide-permeable xerogel is 23-fold greater in comparison to xerogel-free catalyst in solution. The catalyst is easily separated from the reaction mixture via filtration and the recovered catalyst can be reused without loss of activity through formation of the first 80 mol of product per mole of catalyst.
Bennett, Stephanie M.,Tang, Ying,McMaster, Danielle,Bright, Frank V.,Detty, Michael R.
p. 6849 - 6852
(2008/12/22)

New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site
Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of this particular scaffold. Modification to the part of the inhibitor that occupies the adenine/ATP
Moss, Neil,Breitfelder, Steffen,Betageri, Raj,Cirillo, Pier F.,Fadra, Tazmeen,Hickey, Eugene R.,Kirrane, Thomas,Kroe, Rachel R.,Madwed, Jeffrey,Nelson, Richard M.,Pargellis, Christopher A.,Qian, Kevin C.,Regan, John,Swinamer, Alan,Torcellini, Carol
p. 4242 - 4247
(2008/02/09)

{[K.18-Crown-6]Br3}n: a unique tribromide-type and columnar nanotube-like structure for the oxidative coupling of thiols and bromination of some aromatic compounds
Reaction of 18-crown-6 with KBr and then with bromine (Br2) afforded a unique tribromide salt with a nanotube-like structure ({[K.18-crown-6]Br3}n). Oxidative coupling of thiols and bromination of some aromatic compounds is the first report on the chemistry of this reagent.
Zolfigol, Mohammad Ali,Chehardoli, Gholamabbas,Salehzadeh, Sadegh,Adams, Harry,Ward, Michael D.
p. 7969 - 7973
(2008/03/14)

Benzofurans as suppressors of neurodegeneration
A compound of the formula: wherein R1 and R2 each is H or a hydrocarbon group which may be substituted, or R1 and R2 form a 3- to 8-membered carbo or heterocyclic ring which may be substituted; R3 is H, a lower alkyl which may be substituted or an aromatic group which may be substituted; R4 is (1) an aromatic group which may be substituted, (2) an aliphatic hydrocarbon group substituted by an aromatic group which may be substituted, which hydrocarbon group may be further substituted or (3) an acyl; X and Y each is oxygen or sulfur which may be oxidized; and ring A is a benzene ring which may be further substituted, or a salt thereof, is useful for an agent for suppressing neurodegeneration.
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Page/Page column 37

(2010/10/20)

A novel tunable aromatic bromination method using alkyl bromides and sodium hydride in DMSO
Aromatic bromination on various aromatic systems with different substitutions was performed in the presence of alkyl bromide and sodium hydride in DMSO. Mono-bromination on a wide range of substrates was achieved by selecting proper alkyl bromides and controlling its amount. Further bromination could happen with more active alkyl bromides and additional amount of bromides and sodium hydride. The yields ranged from moderate to excellent. In addition, reaction mechanism was postulated to explain our observations.
Guo, MaoJun,Varady, Laszlo,Fokas, Demosthenes,Baldino, Carmen,Yu, Libing
p. 3889 - 3892
(2007/10/03)

Palladium-catalyzed selective amination of haloaromatics on KF-alumina surface
An efficient palladium-catalyzed amination, including polyaminations of aromatic bromides mediated on a surface of KF-alumina, is reported. The solvent-free one-pot protocol avoids the use of a strong base (sodium tert-butoxide) making it applicable to substrates containing a base-sensitive functional group. It proceeds without concomitant reductive bromination and provides access to selective amination of polyhaloaromatics.
Basu, Basudeb,Das, Pralay,Nanda, Ashish K.,Das, Sajal,Sarkar, Sajal
p. 1275 - 1278
(2007/10/03)

NOVEL BENZYL(IDENE)-LACTAM DERIVATIVES
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula (I) wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13, X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.
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Page/Page column 38

(2008/06/13)

CATHEPSIN CYSTEINE PROTEASE INHIBITORS
This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis. They have the following structure: Formula (I).
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Page 66-67

(2010/02/06)

Rho-kinase inhibitors
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
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Page/Page column 77

(2010/02/05)

PYRAZOLE INHIBITORS OF THE TRANSFORMING GROWTH FACTOR
The invention relates to novel pyrazole derivatives of formula (I), which are inhibitors of the transforming growth factor, ("TGF")-? signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase ("ALK")-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
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Page 23

(2010/02/06)

COMPOUNDS
The invention relates to novel imidazopyridine derivatives which are inhibitors of the transforming growth factor, ("TGF")-? signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase ("ALK")-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
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Page 23

(2010/11/30)

2-PHENYLPYRIDIN-4-YL DERIVATIVES AS ALK5 INHIBITORS
This invention relates to novel 2-phenylpyridin-4-yl heterocyclyl derivatives which are inhibitors of the transforming growth factor, ("TGF")-? signalling pathway, in particular, the phosphorylation of smad2 or smad3 by the TGF-β type I or activin-like kinase ("ALK")-5 receptor, methods for their preparation and their use in medicine, specifically in the treatment and prevention of a disease state mediated by this pathway.
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Page 47-48

(2010/02/06)

Microwave-assisted amination from aryl triflates without base and catalyst
(Equation presented) Aryl triflates are effectively converted to the corresponding anilines under microwave irradiation in 1-methyl-2-pyridone (NMP) without base and catalyst. Aryl triflates substituted with both electron-poor and electron-rich groups give good to excellent yields. It is noteworthy that the halogenated aryl triflates can chemoselectively react with amines to afford halogenated anilines.
Xu, Gang,Wang, Yan-Guang
p. 985 - 987
(2007/10/03)