- Metal-Free, Rapid, and Highly Chemoselective Reduction of Aromatic Nitro Compounds at Room Temperature
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In this study, we developed a metal-free and highly chemoselective method for the reduction of aromatic nitro compounds. This reduction was performed using tetrahydroxydiboron [B2(OH)4] as the reductant and 4,4′-bipyridine as the organocatalyst and could be completed within 5 min at room temperature. Under optimal conditions, nitroarenes with sensitive functional groups, such as vinyl, ethynyl, carbonyl, and halogen, were converted into the corresponding anilines with excellent selectivity while avoiding the undesirable reduction of the sensitive functional groups.
- Han, Min Su,Jang, Mingyeong,Lim, Taeho,Park, Byoung Yong
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p. 910 - 919
(2022/01/20)
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- REACTION COMPOSITION AND REACTION SYSTEM USING THIS
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An aromatic nitro compound has a structure in which a nitro group and a halogen atom, in a separated state, are directly bonded as substituents to the ring structure of the same ring; a reaction composition is provided which, in a hydrogenation reaction of the nitro group of said aromatic nitro compound, allows selectively hydrogenating the nitro group, and sufficiently reducing the separation of the halogen atom from the ring; also provided is a reaction system that uses this reaction composition. This reaction composition includes a catalyst which, with the aforementioned aromatic nitro compound as reactant, is used in a hydrogenation reaction of at least one of the one or more nitro groups of said reactant. Further, the reaction composition includes a base and an organic solvent. The catalyst includes a carrier, and Fe oxide particles and Pt particles supported by the carrier.
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Paragraph 0140-0145
(2020/10/10)
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- REACTION COMPOSITION AND REACTION SYSTEM USING THIS
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An aromatic nitro compound has a structure in which a nitro group and a halogen atom, in a separated state, are directly bonded as substituents to the ring structure of the same ring; a reaction composition is provided which, in a hydrogenation reaction of the nitro group of said aromatic nitro compound, allows selectively hydrogenating the nitro group, and sufficiently reducing the separation of the halogen atom from the ring; also provided is a reaction system that uses this reaction composition. This reaction composition includes a solvent, and a catalyst which, with the aforementioned aromatic nitro compound as reactant, is used in a hydrogenation reaction of at least one of the one or more nitro groups of said reactant. The catalyst includes a carrier, and Fe oxide particles and Pt particles supported by the carrier.
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Paragraph 0097-0111
(2020/12/14)
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- CATALYST MIXTURE
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Provided is a catalyst mixture which, in a nitro group hydrogenation reaction of an aromatic nitro compound having a structure in which nitro groups and halogen atoms are directly bonded as substituents to a ring skeleton of the same ring while separated from each other, is capable of selectively hydrogenating the nitro groups and sufficiently reducing the removal of the halogen atoms from the ring. This catalyst mixture includes a catalyst which is used in a hydrogenation reaction of at least one among one or more nitro groups present in a reactant, which is an aromatic nitro compound having a structure in which one or more nitro groups and one or more halogen atoms are directly bonded as substituents to a ring skeleton of the same ring while separated from each other. This catalyst mixture further includes a base.
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Paragraph 0120; 0122-0128
(2020/12/14)
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- Cu-mediated selective bromination of aniline derivatives and preliminary mechanism study
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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
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supporting information
p. 1406 - 1415
(2019/05/01)
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- Synergistic effects in Fe nanoparticles doped with ppm levels of (Pd + Ni). A new catalyst for sustainable nitro group reductions
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A remarkable synergistic effect has been uncovered between ppm levels of Pd and Ni embedded within iron nanoparticles that leads to mild and selective catalytic reductions of nitro-containing aromatics and heteroaromatics in water at room temperature. NaBH4 serves as the source of inexpensive hydride. Broad substrate scope is documented, along with several other features including: low catalyst loading, low residual metal in the products, and recycling of the catalyst and reaction medium, highlight the green nature of this new technology.
- Pang, Haobo,Gallou, Fabrice,Sohn, Hyuntae,Camacho-Bunquin, Jeffrey,Delferro, Massimiliano,Lipshutz, Bruce H.
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supporting information
p. 130 - 135
(2018/01/12)
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- SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Provided is a sulfonamide derivative represented by the following general formula (1) and having an α4 integrin inhibitory effect with high selectivity with a low effect on α4β1 and a high effect on α4β7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).
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Paragraph 0221; 0222; 0223
(2016/09/26)
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- A pyridine primary amine ruthenium complex, preparation method and its use
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The invention relates to a pyridine primary amine ruthenium complex as well as a preparation method and application thereof. The pyridine primary amine ruthenium complex is excellent in anti-cancer activity in anti-cancer screening in vitro and especially has a good inhibition effect on the lung cancer and the human breast cancer, so that the pyridine primary amine ruthenium complex has huge development potential and application value in clinical treatment of tumor diseases.
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Paragraph 0068; 0069
(2017/04/03)
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- BICYCLIC SUBSTITUTED PYRIMIDINE COMPOUNDS
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The present invention relates to the technical field of medicine and pharmacy, and particularly relates to bicyclic group substituted pyrimidine compounds represented by general formula (I), pharmaceutical acceptable salts thereof or stereoisomers thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification. The present invention also relates to preparation methods, pharmaceutical formulations, and pharmaceutical compositions of the compounds, and use of the compounds, pharmaceutical formulations, and pharmaceutical compositions for preparing a medicament for treating and/or preventing sexual dysfuntion diseases and diseases with lower urinay tract symptoms.
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Paragraph 0143; 0144
(2015/07/02)
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- SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
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Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
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Paragraph 1151-1152
(2015/02/25)
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- THREE-RING PI3K AND/OR MTOR INHIBITOR
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The present application relates to a compound as represented by general formula (I), a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, preparation method of the compounds, a pharmaceutical composition containing the compounds, us
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Paragraph 0242; 0243
(2015/06/24)
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- Pyridonaphthyridine PI3K/MTOR Dual Inhibitors and Preparation and Use Thereof
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The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
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Page/Page column
(2014/04/17)
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- PYRIDONAPHTHYRIDINE PI3K/MTOR DUAL INHIBITORS AND PREPARATION AND USE THEREOF
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The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
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Paragraph 0097
(2014/05/07)
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- THREE-RING PI3K AND/OR MTOR INHIBITOR
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The present application relates to a compound as represented by general formula (I), a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, preparation method of the compounds, a pharmaceutical composition containing the compounds, uses thereof in the preparation of drugs for treating and/or preventing proliferative diseases, and a method using the compounds to treat and/or prevent proliferative diseases. R1, R2, R3, R4, R5, R6, X, A and B in the formula are as defined in the specification.
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Paragraph 0102; 0103; 0186 - 0188
(2014/11/11)
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- Selective catalytic hydrogenation of nitro groups in the presence of activated heteroaryl halides
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Chemoselective reduction of nitro groups in the presence of activated heteroaryl halides was achieved via catalytic hydrogenation with a commercially available sulfided platinum catalyst. The optimized conditions employ low temperature, pressure, and catalyst loading (0.1 mol % Pt) to afford heteroaromatic amines with minimal hydrodehalogenation byproducts.
- Kasparian, Annie J.,Savarin, Cecile,Allgeier, Alan M.,Walker, Shawn D.
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experimental part
p. 9841 - 9844
(2012/01/06)
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- Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor
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Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintainin
- Shen, Hong C.,Ding, Fa-Xiang,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Ren, Ning,Cai, Tian-Quan,Deng, Qiaolin,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
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p. 6303 - 6306
(2008/04/12)
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- Pyridine-substituted benzanilides as potassium ion channel openers
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The present invention provides a genus of pyridine-substituted benzanilides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
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- Bisarylamines as potassium channel openers
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Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.
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- Pyridine-substituted benzanilides as potassium ion channel openers
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The present invention provides a genus of pyridine-substituted benzanilides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
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- Mild regioselective halogenation of activated pyridines with N-bromosuccinimide
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Regioselective mono and dihalogenations of amino, hydroxy and methoxy pyridines (2-, 3-, and 4-substituted) as well as 2,6-dimethoxy pyridine with N-bromosuccinimide in different solvents have been studied. Reactivity of the substrates decreases in the order amino>hydroxy>methoxy and regioselectivity depends on the position of the substituent (2-substituted > 3-substituted). In most of the cases we obtained monobrominated derivatives regioselectively and in high yields. Hydroxy and amino pyridines can also be dibrominated in almost quantitative yield with 2 equivalents of NBS.
- Canibano,Rodriguez,Santos,Sanz-Tejedor,Carreno,Gonzalez,Garcia-Ruano
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p. 2175 - 2179
(2007/10/03)
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- 3-Pyridyl enantiomers and their use as analgesics
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The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula I: STR1 or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula I above which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.
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- Furopyridine, thienopyridine pyrrolopyridine useful in controlling chemical synaptic transmission
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Novel heterocyclic ether compounds having the formula: STR1 wherein A, m, R, X, Y1, Y2 and Y3 are specifically defined, which are useful in selectively controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions thereof; and use of said compositions to selectively control synaptic transmission in mammals.
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- Liquid crystal compounds and compositions
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Liquid crystal naphthalene compounds, represented by the following formula (1) are disclosed. R-Z-A- -NAP-Z?-R? (1)In the formula (1), R is an alkyl group containing 1 to 18 carbon atoms; R? is an alkyl group containing 1 to 21 carbon atoms; NAP represents 2,6-naphthylene group; represents C≡C;, A, Z and Z? are as follows: 1) A is Pyr> and, (a) Z is - and Z? is O or COO or (b) Z is OCO and Z? is - or O; 2) A is FPhF and (a) Z is - or O and Z? is -, O or COO or (b) Z is OCO and Z? is - or O; 3) A is FPh and (a) Z is - and Z? is O or COO, (b) Z is O and Z? is -, O or COO or (c) Z is OCO and Z? is - or O; 4) A is Pyr and Z is - or O and Z? is COO; or 5) A is PhF and Z is O and Z? is -; wherein: When used as a component of liquid crystal composition showing ciral smectic C phase, these compounds can provide liquid crystal compositions of improved orientation and free from zigzag deffects, and liquid crystal display elements of high contrast ratio.
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- TITANIUM (O) REAGENTS; 4. A SELECTIVE AND EFFICIENT REDUCTION OF NITROPYRIDINE DERIVATIVES
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Following the successful applications of a titanium (O) slurry in the deoxygenation of aromatic N-oxides, we attempted to achieve this method for the reduction of a nitro- group in pyridine derivatives.In general, only aminopyridine derivates were formed in 85-98percent yield.The advantage of this excellent reducing agent consists in mild reaction conditions and high yields of products, as well as in the selectivity of the reaction.
- Malinowski, Marek
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