- Mild Darzens Annulations for the Assembly of Trifluoromethylthiolated (SCF3) Aziridine and Cyclopropane Structures
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We report mild new annulation approaches to trisubstituted trifluoromethylthiolated (SCF3) aziridines and cyclopropanes via Darzens inspired protocols. The products of these anionic annulations, rarely studied previously, possess attractive features rendering them valuable building blocks for synthesis platforms. In this study, trisubstituted acetophenone nucleophiles bearing SCF3 and bromine substituents in their α position were shown to undergo [2 + 1] annulations with vinyl ketones and tosyl-protected imines under mild reaction conditions.
- Delost, Michael D.,Njardarson, Jon T.
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supporting information
p. 6121 - 6125
(2021/08/16)
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- INHIBITORS OF DNA GYRASE FOR THE TREATMENT OF BACTERIAL INFECTIONS
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The present invention relates to compounds which specifically inhibit bacterial DNA Gyrase and can be used for the treatment of respiratory tract infections.
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Page/Page column 44
(2014/05/07)
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- Copper- and silver-mediated cyanation of aryl iodides using ddq as cyanide source
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A new copper and silver-mediated cyanation of aryl iodides with DDQ as a cyanide source is achieved, providing nitriles with good yields. This new approach represents a safe method leading to aryl nitriles. A new copper and silver-mediated cyanation of aryl iodides with DDQ as a cyanide source is achieved.
- Zheng, Kui,Yu, Peng,Chen, Shuyou,Chen, Fen,Cheng, Jiang
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supporting information
p. 449 - 452
(2013/08/25)
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- One pot synthesis of nitriles from aldehydes and hydroxylamine hydrochloride using ferrous sulphate in DMF under reflux condition
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A rapid and facile one pot synthesis of nitrile has been carried out in high yields from the corresponding aldehydes and hydroxylamine hydrochloride in the presence of anhydrous ferrous sulphate and DMF under reflux condition.
- Patil, Dinanath D.,Wadhava, Gurumeet C.,Deshmukh, Arun K.
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experimental part
p. 1401 - 1402
(2012/08/28)
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- Quinoxaline compounds
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Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
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Page/Page column 29
(2008/06/13)
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- Progress in the palladium-catalyzed cyanation of aryl chlorides
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The development of new palladium catalysts for the cyanation of various aryl and heteroaryl chlorides is described. The combination of amine co-catalysts with chelating phosphine ligands, for example, 1,4-bis(diphenylphosphino)butane (dppb) or 1,5-bis(diphenylphosphino)pentane (dpppe), allows an efficient cyanation of chloroarenes with simple potassium cyanide. General palladium-catalyzed cyanation of nonactivated and deactivated chloroarenes is possible for the first time. Studies of the oxidative addition of aryl halides to palladium triphenylphosphine complexes in the presence and absence of amines suggest that the co-catalyst is capable of preventing catalyst deactivation caused by the presence of excess cyanide ions in solution.
- Sundermeier, Mark,Zapf, Alexander,Mutyala, Sateesh,Baumann, Wolfgang,Sans, Juergen,Weiss, Stefan,Beller, Matthias
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p. 1828 - 1836
(2007/10/03)
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- Nitration of moderately deactivated arenes with nitrogen dioxide and molecular oxygen under neutral conditions. Zeolite-induced enhancement of regioselectivity and reversal of isomer ratios
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In the presence of zeolites, moderately deactivated arenes such as 1-nitronaphthalene, naphthonitriles, and methylated benzonitriles can be smoothly nitrated at room temperature by the combined action of nitrogen dioxide and molecular oxygen. The regioselectivity is considerably improved as compared with the conventional nitration methodology based on nitric and sulfuric acids. In some cases, the minor isomer became favoured to a significant extent, resulting in the reversal of ordinary isomer ratios of nitration products.
- Peng, Xinhua,Fukui, Naoyuki,Mizuta, Masayuki,Suzuki, Hitomi
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p. 2326 - 2335
(2007/10/03)
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- Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-monocyclic arginine surrogates
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Investigations on P2-P3-heterocyclic dipeptide surrogates directed towards identification of an orally bioavailable thrombin inhibitor led us to pursue novel classes of achiral, non-covalent P1-arginine derivatives. The design, synthesis, and biological activity of inhibitors NC1-NC30 that feature three classes of monocyclic P1-arginine surrogates will be disclosed: (1) (hetero)aromatic amidines, amines and hydroxyamidines, (2) 2-aminopyrazines, and (3) 2-aminopyrimidines and 2-aminotetrahydropyrimidines.
- Reiner, John E.,Siev, Daniel V.,Araldi, Gian-Luca,Cui, Jingrong Jean,Ho, Jonathan Z.,Reddy, Komandla Malla,Mamedova, Lala,Vu, Phong H.,Lee, Kuen-Shan S.,Minami, Nathaniel K.,Gibson, Tony S.,Anderson, Susanne M.,Bradbury, Annette E.,Nolan, Thomas G.,Semple, J. Edward
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p. 1203 - 1208
(2007/10/03)
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- Piperazine compounds and medicinal use thereof
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The present invention relates to a piperazine compound of the formula wherein R1and R2are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4and R5are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6and R7are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8and R9are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.
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- Thrombin inhibitors, the preparation and use thereof
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Compounds of the formula and the salts thereof with physiologically tolerated acids and the stereoisomers thereof, in which the substituents have the meanings stated in the description, are described. Also disclosed are intermediates for their preparation. The compounds are suitable for controlling diseases.
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- Aromatic amidine derivatives useful as selective thrombin inhibitors
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The present invention relates to a novel thrombin inhibitor which is effective even when orally administered. More specifically, the present invention relates to an aromatic amidine derivative represented by formula (I) and the salts thereof, which show potent selective inhibitory activity for thrombin in which (a), R, R1, R2, R3, A, W, Y and n are defined as described in the specification.
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- Formamide assisted one-pot conversion of aromatic aldehydes into the corresponding nitriles1
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A single step conversion of aromatic aldehydes (1) into the corresponding nitriles (2) has been achieved in high yields using stoichiometric amounts of hydroxylamine hydrochloride, pyridine and formamide in refluxing xylene.
- Ali, Sayyed Iliyas,Nikalje, Milind D.,Dewkar, Gajanan K.,Paraskar, Abhimanyu S.,Jagtap,Sudalai
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- Thrombin inhibitors
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Thrombin inhibitors of the formula STR1 where R 1, A, B and D have the meaning indicated in the description, and intermediates for the preparation thereof are described.The compounds I are suitable for controlling diseases.
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- The scope and limitations of cyanide groups as direction labels for the conformational analysis of matrix-isolated molecules of low symmetry Part 2: 3-Cyanophenyl azide and two conformationally restrained derivatives
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3-Cyanophenyl azide and derivatives with ortho methyl groups were photolysed with plane-polarized light in N2 matrices at 12-20 K. The resulting matrices containing the methyl-substituted derivatives had pronounced IR linear dichroism, which wa
- Dunkin,Shields
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p. 141 - 150
(2007/10/03)
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- C-Azidodiazirines in the SRN1 Reaction of Azide Ion with Arylchlorodiazirines. Further Insights into Reaction Mechanism
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Mixtures of arylchlorodiazirines and sodium azide in DMSO form visible charge transfer complexes.Irradiation of these solutions with fluorescent room light leads to SRN1 displacement of chloride and the transient formation of C-azidodiazirines.Relative reactivity studies (using competition experiments) show that nitro-substituted arylchlorodiazirines are substantially more reactive than other arylchlorodiazirines.This is attributed to facile electron transfer in the propagation cycle, involving the nitro-substituted aromatic ring.C-Azidodiazirines can be isolatedin solution and spectroscopically characterized when the SRN1 reaction is initiated by addition of catalytic amounts of the sodium salt of 2-nitropropane.These azidodiazirines readily decompose at room temperature by first order processes to give molecular nitrogen and benzonitriles.Solvent and substituent effects on decomposition rates are minimal.Computational studies on potential intermediate carbenes in the decomposition of azidodiazirines have been carried out at the HF/6-31-G* level.Singlet α-azidocarbenes RCN3, where R = NH2, OH, F, vinyl, phenyl, and CH3, are energy minima at this computational level.Isodesmic calculations show that the azido group is comparable to OH in its carbene stabilizing ability.Subsequent loss of N2 from α-azidocarbenes, leading to nitriles, is a highly exothermic process (126 kcal when R = vinyl and 128 kcal when R = phenyl).
- Creary, Xavier
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p. 7700 - 7708
(2007/10/02)
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- 1-Alkyl-2-isocyanatomethyl-isocyanatobenzenes and/or 1-alkyl-4-isocyanatomethyl-isocyanatobenzenes
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The invention describes new aromatic diisocyanates having the formulas: STR1 in which R is an alkyl radical with 1 to 12 carbon atoms. Preferably they are 1-alkyl-2-isocyanatomethyl-4-isocyanatobenzenes and/or 1-alkyl-4-isocyanatomethyl-2-isocyanatobenzen
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- Antiprotozoal diamidines
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Diamidines of the formula STR1 wherein X is a propylene, isobutylene, guanidine, pyrrole, tetrazole, imidazole or substituted imidazole group; and 2-[4-(2-imidazolinyl)phenyl]-6-(2-imidazolinyl)indole, are useful in the treatment of certain protozoal infections in mammals, particularly in cattle.
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