- Investigation on Factors Ruling Catalytic Efficiency and Chemical Stability of Mn(III) Porphyrins in HOCl Olefin Epoxidation: Conditions for Practical Applications
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The use of stable Mn(III) porphyrins (P), e.g. 2-4, and of imidazole or pyridine axial ligands (L), 8-10, entirely soluble in the organic phase has allowed an extensive investigation of the factors ruling the catalytic activity of porphyrins in the olefin
- Banfi, Stefano,Montanari, Fernando,Quici, Silvio
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- 2-Position-selective C[sbnd]H fluoromethylation of six-membered heteroaryl N-oxides with (fluoromethyl)triphenylphosphonium iodide
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A mild and efficient method for the regioselective C[sbnd]H fluoromethylation of heteroaryl N-oxides with (fluoromethyl)triphenylphosphonium iodide is presented. With LiOt-Bu as the base and DMSO as the solvent, this reaction delivers a series of C2-fluor
- Hu, Chen-Chen,Hu, Wei-Qiang,Qing, Feng-Ling,Xu, Xiu-Hua
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- An efficient Pd(II)-(2-aminonicotinaldehyde) complex as complementary catalyst for the Suzuki-Miyaura coupling in water
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An efficient new Pd(II)-(2-aminonicotinaldehyde)-catalyzed Suzuki-Miyaura coupling of the aryl halides (Br, Cl and I) and organoboronic acids at moderate temperature in water is described. Low catalyst loading, easy accessibility, being an air-stable catalyst, functional group compatibility, and water as the reaction medium are some of the key features of this synthetic method. This protocol is also applicable for gram scale.
- Thunga, Sanjeeva,Poshala, Soumya,Anugu, Naveenkumar,Konakanchi, Ramaiah,Vanaparthi, Satheesh,Kokatla, Hari Prasad
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supporting information
p. 2046 - 2048
(2019/07/04)
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- Nickel-catalyzed C–H trifluoromethylation of pyridine N-oxides with Togni's reagent
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The first nickel-catalyzed C–H trifluoromethylation of pyridine N-oxides with Togni's reagent has been achieved. Trifluoromethylation proceeds smoothly under mild conditions with moderate functional group compatibility. Notable advantages of this method include the using of low cost of nickel catalyst, and its simple convenient operation.
- Gao, Xianying,Geng, Yang,Han, Shuaijun,Liang, Apeng,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
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supporting information
p. 1551 - 1554
(2018/03/23)
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- 2,2′-Homocoupled Azine N,N′-Dioxides or Azine N-Oxides: CDC- or SNAr-Controlled Chemoselectivity
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An unprecedented Cu(OAc)2- and LiOtBu-mediated homocoupling of azine N-oxides to yield 2,2′-azine N,N′-dioxides is reported. This is the first instance in which copper has been used to catalyze the homodimerization reaction, especially of 2-phenylpyridine N-oxides. In the absence of catalytic copper, the reaction follows an alternative pathway, and instead of dioxides it yields 2,2′-azine N-monoxides. This latter protocol works efficiently with a range of N-heterocyclic oxides of pyridine, 2-phenylpyridine, quinoline and N-aryl-1,2,3-triazole. It is scalable, offers high regioselectivity and gives the products in moderate to high yields. The observed chemoselectivity between the copper-assisted and copper-free protocols is routed through oxidative cross-dehydrogenative coupling (CDC) and nucleophilic aromatic substitution of hydrogen (SNAr) pathways, respectively.
- Jha, Abadh Kishor,Jain, Nidhi
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p. 4765 - 4772
(2017/09/07)
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- The microwave-assisted ortho-alkylation of azine N-oxides with N-tosylhydrazones catalyzed by copper(i) iodide
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A copper catalyzed regioselective cross-coupling of N-tosylhydrazones with azine N-oxides to yield ortho-alkylated products in moderate to good yields is reported. The reaction is facilitated by microwave, takes place without any ligand, and uses inexpensive copper(i) iodide as the catalyst.
- Jha, Abadh Kishor,Jain, Nidhi
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supporting information
p. 1831 - 1834
(2016/02/05)
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- Arylation of pyridine N-oxides via a ligand-free Suzuki reaction in water
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We report a practical and highly efficient protocol for the arylation of pyridine N-oxides with arylboronic acid through palladium-catalyzed Suzuki reaction in water. This ligand-free Suzuki reaction is performed in the presence of diisopropylamine and gi
- Liu, Chun,Zhang, Shao-Ke,Zhang, Yi-Xia,Jin, Zi-Lin
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- Insights into the mechanistic and synthetic aspects of the Mo/P-catalyzed oxidation of N-heterocycles
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A Mo/P catalytic system for an efficient gram-scale oxidation of a variety of nitrogen heterocycles to N-oxides with hydrogen peroxide as terminal oxidant has been investigated. Combined spectroscopic and crystallographic studies point to the tetranuclear Mo4P peroxo complex as one of the active catalytic species present in the solution. Based on this finding an optimized catalytic system has been developed. The utility and chemoselectivity of the catalytic system has been demonstrated by the synthesis of over 20 heterocyclic N-oxides.
- Larionov, Oleg V.,Stephens, David,Mfuh, Adelphe M.,Arman, Hadi D.,Naumova, Anastasia S.,Chavez, Gabriel,Skenderi, Behije
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p. 3026 - 3036
(2014/05/06)
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- NOVEL DXR INHIBITORS FOR ANTIMICROBIAL THERAPY
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The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particuarl embodiments, the compositions target DXR. In specific embodiments, the compositions are electron-deficient heterocyclic rings.
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Page/Page column 69; 75
(2011/05/05)
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- Coordination chemistry based approach to lipophilic inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase
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1-Deoxy-D-xylulose-5-phosphate reductoisomerase (DXR) in the non-mevalonate pathway found in most bacteria is a validated anti-infective drug target. Fosmidomycin, a potent DXR inhibitor, is active against Gram-negative bacteria. A coordination chemistry and structure based approach was used to discover a novel, lipophilic DXR inhibitor with an IC50 of 1.4 μM. It exhibited a broad spectrum of activity against Gram-negative and -positive bacteria with minimal inhibition concentrations of 20-100 μM (or 3.7-19 μg/mL).
- Deng, Lisheng,Sundriyal, Sandeep,Rubio, Valentina,Shi, Zheng-Zheng,Song, Yongcheng
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supporting information; experimental part
p. 6539 - 6542
(2010/04/04)
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- 2-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-3-PHENYL PYRAZINES AND PYRIDINES AND 3-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-2-PHENYL PYRIDINES AS 5-HT7 RECEPTOR ANTAGONISTS
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The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)= or N=, provided that at least one of A and B is -N=, n is 1-3, m is 0-3, and R14 are as defined herein.
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Page/Page column 48
(2009/01/20)
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- 2-Aminomethyl piperidines as novel urotensin-II receptor antagonists
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A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent, cross-species active, and functional urotensin-II receptor antagonists such as 1a and 11a are described.
- Jin, Jian,Wang, Yonghui,Wang, Feng,Shi, Dongchuan,Erhard, Karl F.,Wu, Zining,Guida, Brian F.,Lawrence, Sarah K.,Behm, David J.,Disa, Jyoti,Vaidya, Kalindi S.,Evans, Christopher,McMillan, Lynette J.,Rivero, Ralph A.,Neeb, Michael J.,Douglas, Stephen A.
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p. 2860 - 2864
(2008/12/22)
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- Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: Preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods
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New analogues of the previously described 3-aryl pyridone KOR agonists have been synthesised by parallel synthetic methods, both in solution- and with solid-phase chemistry, making use of the well known and versatile Mitsunobu, Suzuki and Buchwald reactions. Opioid receptor binding data for the compounds produced is reported.
- Semple, Graeme,Andersson, Britt-Marie,Chhajlani, Vijay,Georgsson, Jennie,Johansson, Magnus J.,Rosenquist, Asa,Swanson, Lars
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p. 1141 - 1145
(2007/10/03)
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- 3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists
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A new series of 3-aryl pyridone based kappa opioid receptor agonists was designed and synthesised, based on an understanding of the classical kappa opioid receptor pharmacophore. The most potent of the new compounds were comparable to U-69,593 in receptor affinity, selectivity and functional agonist effect at the cloned human kappa opioid receptor.
- Semple, Graeme,Andersson, Britt-Marie,Chhajlani, Vijay,Georgsson, Jennie,Johansson, Magnus,Lindschoten, Marcel,Ponten, Fritof,Rosenquist, Asa,Soerensen, Henrik,Swanson, Lars,Swanson, Marianne
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p. 197 - 200
(2007/10/03)
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