- Yeast supported gold nanoparticles: an efficient catalyst for the synthesis of commercially important aryl amines
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Candida parapsilosisATCC 7330 supported gold nanoparticles (CpGNP), prepared by a simple and green method can selectively reduce nitroarenes and substituted nitroarenes with different functional groups like halides (-F, -Cl, -Br), olefins, esters and nitriles using sodium borohydride. The product aryl amines which are useful for the preparation of pharmaceuticals, polymers and agrochemicals were obtained in good yields (up to >95%) using CpGNP catalyst under mild conditions. The catalyst showed high recyclability (≥10 cycles) and is a robust free flowing powder, stored and used after eight months without any loss in catalytic activity.
- Krishnan, Saravanan,Patel, Paresh N.,Balasubramanian, Kalpattu K.,Chadha, Anju
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supporting information
p. 1915 - 1923
(2021/02/06)
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- Development of a novel protocol for chemoselective deprotection of N/O-benzyloxycarbonyl (Cbz) at ambient temperature
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Abstract: A novel protocol for the deprotection of N-benzyloxycarbonyl and O-benzyloxycarbonyl groups by nickel boride generated in situ from NaBH4 and NiCl2·6H2O in methanol at room temperature has been developed to give the corresponding amines and phenols. This protocol is chemoselective as groups like chloro, bromo, amide, ester, pyridine, and tert-butyloxycarbonyl moiety are unaffected under these conditions. The deprotection has also been validated in gram scale reactions, to establish the wider appropriateness of this protocol. Graphical abstract: [Figure not available: see fulltext.].
- Saroha, Mohit,Aggarwal, Komal,Bartwal, Gaurav,Khurana, Jitender M.
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p. 2231 - 2235
(2018/10/02)
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- Application of Silicon-Initiated Water Splitting for the Reduction of Organic Substrates
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The use of water as a donor for hydrogen suitable for the reduction of several important classes of organic compounds is described. It is found that the reductive water splitting can be promoted by several metalloids among which silicon shows the best efficiency. The developed methodologies were applied for the reduction of nitro compounds, N-oxides, sulfoxides, alkenes, alkynes, hydrodehalogenation as well as for the gram-scale synthesis of several substrates of industrial importance.
- Gevorgyan, Ashot,Mkrtchyan, Satenik,Grigoryan, Tatevik,Iaroshenko, Viktor O.
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p. 375 - 382
(2018/06/04)
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- Synthesis of novel ethyl 1-ethyl-6-fluoro-7-(fatty amido)-1,4-dihydro-4-oxoquinoline-3-carboxylate derivatives and their biological evaluation
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A series of novel ethyl 1-ethyl-6-fluoro-7-(fatty amido)-1,4-dihydro-4-oxoquinoline-3-carboxylate derivatives were prepared through multistep synthesis. The key step in the synthesis was to obtain the C-7 fatty amide derivative. The azide was selectively formed at C-7 position using sodium azide at 60 °C. Subsequently, the azide was reduced under mild conditions using zinc and ammonium chloride to form the corresponding amine. The synthesized derivatives were further subjected to biological evaluation studies like cytotoxicity against a panel of cancer cell lines such as DU145, A549, SKOV3, MCF7 and normal lung cells, IMR-90 as well as with antimicrobial and antioxidant activities. It was observed that the carboxylated quinolone derivatives with hexanoic (8a), octanoic (8b), lauric (8d) and myristic (8e) moieties exhibited promising cytotoxicity against all the tested cancer cell lines. The results also suggested that hexanoic acid-based fatty amide carboxylated quinolone derivative (8a) exhibited promising activity against both bacterial and fungal strains and significant antibacterial activity was observed against Staphylococcus aureus MTCC 96 (MIC value of 3.9 μg/mL). The compound 8a also showed excellent anti-biofilm activity against Staphylococcus aureus MTCC 96 and Bacillus subtilis MTCC 121 with MIC values of 2.1 and 4.6 μg/mL, respectively.
- Venepally, Vijayendar,Prasad,Poornachandra,Kumar, C. Ganesh,Jala, Ram Chandra Reddy
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supporting information
p. 613 - 617
(2016/01/09)
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- NOVEL OXAZOLIDINONE COMPOUNDS
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A novel oxazolidinone compound (S)-N-((3-(4-fluoro-3-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl)acetamide of formula -I and a process for the preparation thereof. Compound-I.
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Page/Page column 9; 16
(2015/05/26)
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- Dialkylimidazole inhibitors of Trypanosoma cruzi sterol 14α-demethylase as anti-Chagas disease agents
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New dialkylimidazole based sterol 14α-demethylase inhibitors were prepared and tested as potential anti-Trypanosoma cruzi agents. Previous studies had identified compound 2 as the most potent and selective inhibitor against parasite cultures. In addition, animal studies had demonstrated that compound 2 is highly efficacious in the acute model of the disease. However, compound 2 has a high molecular weight and high hydrophobicity, issues addressed here. Systematic modifications were carried out at four positions on the scaffold and several inhibitors were identified which are highly potent (EC50 1 nM) against T. cruzi in culture. The halogenated derivatives 36j, 36k, and 36p, display excellent activity against T. cruzi amastigotes, with reduced molecular weight and lipophilicity, and exhibit suitable physicochemical properties for an oral drug candidate.
- Suryadevara, Praveen Kumar,Racherla, Kishore Kumar,Olepu, Srinivas,Norcross, Neil R.,Tatipaka, Hari Babu,Arif, Jennifer A.,Planer, Joseph D.,Lepesheva, Galina I.,Verlinde, Christophe L.M.J.,Buckner, Frederick S.,Gelb, Michael H.
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supporting information
p. 6492 - 6499
(2013/11/19)
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- Highly efficient chemoselective N-TBS protection of anilines under exceptional mild conditions in the eco-friendly solvent 2-methyltetrahydrofuran
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A straightforward chemoselective protection of anilines as N-TBS derivatives is described by using a suitable deprotonation of the amine with methyllithium in the environmentally friendly and safer substitute of THF, 2-methyltetrahydrofuran, under exceptional mild reaction conditions (0 °C, 30 min). Interestingly, the protecting group maybe cleaved efficiently by simple treatment of N-TBS-anilines with silica gel in ethanol-water.
- Pace, Vittorio,Alcantara, Andres R.,Holzer, Wolfgang
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supporting information; experimental part
p. 1986 - 1989
(2011/09/16)
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- Rapid reduction of heteroaromatic nitro groups using catalytic transfer hydrogenation with microwave heating
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A method for the rapid, safe reduction of heteroaromatic and aromatic nitro groups to amines is described using catalytic transfer hydrogenation under microwave heating conditions. Commonly available Pd/C or Pt/C catalyst is extremely effective with 1,4-cyclohexadiene as the hydrogen transfer source. In the case of substrates containing potentially labile aromatic halogens, Pt/C is effective and results in little or no dehalogenation. In general, the reactions are complete within 5 min at 120 °C.
- Quinn, John F.,Bryant, Cole E.,Golden, Kathryn C.,Gregg, Brian T.
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experimental part
p. 786 - 789
(2010/03/24)
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- Electrophilic aromatic fluorination with fluorine: meta-Directed fluorination of anilines
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Anilines are mainly or selectively fluorinated in the meta-position with F2 when dissolved in triflic acid, sometimes in the presence of small quantities of antimony pentafluoride. The regioselectivity is increased when an electron-donating substituent is present at the para-position.
- Alric,Marquet,Billard,Langlois
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p. 661 - 667
(2007/10/03)
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- Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
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A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
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- ARYL SULFONAMIDES
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Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
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- New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
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A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Indium Mediated Reduction of Nitro and Azide Groups in the Presence of HCl in Aqueous Media
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Indium mediated reduction of azide and nitro groups in the presence of HCl (1.5 equiv based on indium) at room temperature in aqueous THF successfully provided the corresponding amine in high to quantitative yields. Under the some reaction conditions, selective reduction of azide and nitro group in the presence of vinyl group could be accomplished.
- Lee, Jung Gyu,Choi, Kyung Il,Koh, Hun Yeong,Kim, Youseung,Kang, Yonghan,Cho, Yong Seo
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- Camptothecin analogues, preparation methods therefor, use thereof as drugs, and pharmaceutical compositions containing said analogues
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A camptothecin analog characterized in that the hydroxy lactone of the camptothecin is a β-hydroxy lactone or the corresponding β-hydroxyacid, resulting from the opening of said lactone, or a derivative of said β-hydroxyacid, or a Pharmaceutically acceptable salt thereof, is disclosed. In particular, compounds of formulae (I) and (II) are disclosed. Methods for preparing the compounds of formulae (I) and (II), pharmaceutical compositions containing said containing said compounds, and their use, particularly as topoisomerase inhibitors and antitumoral drugs, are also disclosed.
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- Process for producing chlorofluorobenzenes
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A process for producing chlorofluorobenzenes, which comprises reacting fluorine-containing nitrobenzenes of the following formula (1) with chlorine gas to obtain chlorofluorobenzenes of the following formula (2): STR1 wherein n and m are integers satisfying 1≤n≤3, 0≤m≤2 and 1≤n+m≤3.
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- General and Highly Efficient Syntheses of m-Fluoro Arenes Using Potassium Fluoride-Exchange Method
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Tetraphenylphosphonium bromide was found to be a suitable catalyst for the reaction of m-nitroaryl derivatives carrying cyano, nitro, chlorocarbonyl, trifluoromethyl, and chlorosulfonyl groups with potassium fluoride in the presence of a stoichiometric amount of phthaloyl dichloride, giving the corresponding m-fluoro aromatic derivatives in good yields.The catalyst was also found to be efficient for the fluorodesulfonylation of m-(fluorosulfonyl)aryl derivatives to afford m-fluoro arenes by the use of a reaction-distillation technique.
- Suzuki, Hiroshi,Yazawa, Naoto,Yoshida, Yasuo,Furusawa, Osamu,Kimura, Yoshikazu
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p. 2010 - 2017
(2007/10/02)
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- SYNTHESIS AND SOME PROPERTIES OF 3,4-DIFLUOROPHENYL TRANS-4 prime -SUBSTITUTED CYCLOHEXANE-1 prime -CARBOXYLATES.
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A new series of 3,4-difluorophenyl trans-4 prime -substituted cyclohexane-1 prime -carboxylates was synthesized in order to achieve a nematic compound of positive dielectric anisotropy and low viscosity. The effect of fluoro substituents on mesomorphic and physical properties was established by comparing these compounds with other fluorinated nematic compounds.
- Takatsu,Takeuchi,Sato
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p. 165 - 180
(2007/10/02)
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- Method for the preparation of fluoroaniline
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A process for the preparation of fluoroaniline compounds comprises the steps of (A) reacting an ammonium fluorophthalamate or a fluorophthalamic acid of the formula STR1 where n is 1 or 2 with an alkali or an alkali earth metal hypochlorite to form the corresponding fluoroanthranilic acid; and (B) decarboxylating the fluoroanthranilic acid by reaction with a mineral acid to form the corresponding fluoroaniline of the formula STR2 where n is as previously defined.
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- 4- and 5-Substituted 2,3-dihydro-1H-isoindoles, pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase
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Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using novel 2,3-dihydro-1H-isoindole compounds having 4- and 5-substituents.
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