- Visible-light assisted of nano Ni/g-C3N4 with efficient photocatalytic activity and stability for selective aerobic C?H activation and epoxidation
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A selective, economical, and ecological protocol has been described for the oxidation of methyl arenes and their analogs to the corresponding carbonyl compounds and epoxidation reactions of alkenes with molecular oxygen (O2) or air as a green oxygen source, under mild reaction conditions. The nano Ni/g-C3N4 exhibited high photocatalytic activity, stability, and selectivity in the C?H activation of methyl arenes, methylene arenes, and epoxidation of various alkenes under visible- light irradiation without the use of an oxidizing agent and under base free conditions.
- Akrami, Zahra,Hosseini-Sarvari, Mona
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supporting information
(2020/10/13)
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- On/Off O2 Switchable Photocatalytic Oxidative and Protodecarboxylation of Carboxylic Acids
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Photoredox catalysis in recent years has manifested a powerful branch of science in organic synthesis. Although merging photoredox and metal catalysts has been a widely used method, switchable heterogeneous photoredox catalysis has rarely been considered. Herein, we open a new window to use a switchable heterogeneous photoredox catalyst which could be turned on/off by changing a simple stimulus (O2) for two opponent reactions, namely, oxidative and protodecarboxylation. Using this strategy, we demonstrate that Au@ZnO core-shell nanoparticles could be used as a switchable photocatalyst which has good catalytic activity to absorb visible light due to the localized surface plasmon resonance effect of gold, can decarboxylate a wide range of aromatic and aliphatic carboxylic acids, have multiple reusability, and are a reasonable candidate for synthesizing both aldehydes/ketones and alkane/arenes in a large-scale set up. Some biologically active molecules are also shown via examples of the direct oxidative and protodecarboxylation which widely provided pharmaceutical agents.
- Bazyar, Zahra,Hosseini-Sarvari, Mona
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p. 13503 - 13515
(2019/10/11)
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- Iterative design of a biomimetic catalyst for amino acid thioester condensation
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Herein, the design of a catalyst that combines lessons learned from peptide biosynthesis, enzymes, and organocatalysts is described. The catalyst features a urea scaffold for carbonyl recognition and elements of nucleophilic catalysis. In the presence of 10 mol % of the organocatalyst, the rate of peptide bond formation is accelerated by 10000-fold over the uncatalyzed reaction between Fmoc-amino acid thioesters and amino acid methyl esters.
- Wu, Huabin,Handoko,Raj, Monika,Arora, Paramjit S.
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supporting information
p. 5122 - 5125
(2017/11/06)
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- General synthetic strategies towards N-alkyl sulfoximine building blocks for medicinal chemistry and the use of dimethylsulfoximine as a versatile precursor
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The sulfoximine group has great potential as a substituent in drug discovery, as evidenced by two new clinical candidates, and can be viewed as an isosteric alternative to the commonly used sulfone. Our aim was to improve the accessibility of this group by synthesising a diverse range of S-alkyl and N-alkyl sulfoximine building blocks with procedures that are applicable on a practical scale (>10 g). In particular, synthesis of the less well exploited N-alkyl sulfoximines and the use of dimethylsulfoximine as a versatile, commercially available precursor is discussed.
- Goldberg, Frederick W.,Kettle, Jason G.,Xiong, Jian,Lin, Daoguang
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p. 6613 - 6622
(2015/03/30)
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- Novel pseudopeptides incorporating a benzodiazepine-based turn mimetic - Targeting Mycobacterium tuberculosis ribonucleotide reductase
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Peptides mimicking the C-terminus of the small subunit (R2) of Mycobacterium tuberculosis ribonucleotide reductase (RNR) can compete for binding to the large subunit (R1) and thus inhibit RNR activity. Moreover, it has been suggested that the binding of t
- Nurbo, Johanna,Ericsson, Daniel J.,Rosenstr?m, Ulrika,Muthas, Daniel,Jansson, Anna M.,Lindeberg, Gunnar,Unge, Torsten,Karlén, Anders
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p. 1992 - 2000
(2013/05/08)
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- OXO-HETEROCYCLIC SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AND THE USE THEREOF
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The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
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Page/Page column 101; 102
(2011/02/26)
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- Carbazole inhibitors of histamine receptors for the treatment of disease
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The present invention relates to carbazole compounds, pharmaceutical compositions comprising them, and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 72
(2012/01/04)
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- New selective AT2 receptor ligands encompassing a γ-turn mimetic replacing the amino acid residues 4-5 of angiotensin II act as agonists
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New benzodiazepine-based γ-turn mimetics with one or two amino acid side chains were synthesized. The γ-turn mimetics were incorporated into angiotensin II (Ang II) replacing the Val3-Tyr4-Ile 5 or Tyr4-Ile
- Rosenstr?m, Ulrika,Sk?ld, Christian,Plouffe, Bianca,Beaudry, Hélène,Lindeberg, Gunnar,Botros, Milad,Nyberg, Fred,Wolf, Gunter,Karlén, Anders,Gallo-Payet, Nicole,Hallberg, Anders
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p. 4009 - 4024
(2007/10/03)
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- Compounds useful in treating cytokine mediated diseases
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Disclosed are amide compounds of formula(I): wherein Ar1, Q, Y and R3-R6 of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating d
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- 4-Imidazole derivatives of benzyl and restricted benzyl sulfonamides, sulfamides, ureas, carbamates, and amides and their use
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Compounds of formula I are useful in treating diseases prevented by or ameliorated with α1A agonists. Also disclosed are α1A agonist compositions and a method of activating α1 adrenoceptors in a mammal.
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- Preparation and NMR analysis of 2,6-heterodifunctional halobenzenes as precursors for substituted biphenyls
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Preparation and complete characterization of 16 2,6-disubstituted halobenzenes, including nine new compounds, from two common starting materials is described. Seven of the new compounds contain one or two propylthio groups, which have been introduced in two ways. Direct reaction of arenediazonium salts with 1-propanethiolate gives yields comparable to those obtained in a three-step method through sulfonyl chlorides. The 1H- and 13C NMR chemical shifts of 17 1,2,3-trisubstituted benzenes have been correlated with the predicted values and the observed trends explained using commonly available modeling packages.
- Sienkowska, Monika,Benin, Vladimir,Kaszynski, Piotr
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p. 165 - 173
(2007/10/03)
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- Synthesis and antihypertensive activity of 1,4-dihydropyridine derivatives with a 4-(disubstituted phenyl) ring and an aminoalkyl ester group: Highly potent and long-lasting calcium antagonists
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New 1,4-dihydropyridine derivatives bearing a 4-(disubstituted phenyl) ring and an aminoethyl ester or an amino-2,2-dimethylpropyl ester were synthesized and their antihypertensive activities were examined in normotensive rats and spontaneously hypertensi
- Kanno,Yamaguchi,Okamiya,Sunakawa,Takeshita,Naruchi
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p. 2049 - 2054
(2007/10/02)
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- Studies directed toward ascertaining the active conformation of 1,4-dihydropyridine calcium entry blockers
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A series of unsymmetrically substituted 4-phenyl-1,4-dihydropyridine calcium entry blockers were investigated for their ability to relax potassium-contracted rabbit aortic smooth muscle and to competitively displace [3H][nitrendipine from its specific binding sites on guinea pig myocardial membranes in order to delineate the pharmacologically active conformer with respect to the position of the aromatic substituents (synperiplanar or antiperiplanar). The data show that the 1,4-dihydropyridine receptor distinguishes between 2',3'-disubstituted phenyldihydropyridines and 2',5'-disubstituted analogues as measured by changes of vasodilation and receptor affinity in vitro. The IC50 values for vasorelaxation by the analogues presented here correlate best with the K(d) values for binding to the predominant receptor of two coexisting dihydropyridine binding sites in the guinea pig myocardium. We report the first observation of an antiperiplaner orientation of an o-phenyl substituent in the X-ray structure of 2-chlorophenyl analogue 3. Using nuclear Overhauser enhancement, we have developed a method that also demonstrates that an ortho (chloro or nitro) substituent on the phenyl ring does not preclude the presence of either synperiplanar or antiperiplanar phenyl rotamer in solution. These experimental findings contrast with the accepted belief that o-phenyl substituents essentially force these 1,4-dihydropyridines into the synperiplanar conformation exclusively.
- Rovnyak,Andersen,Gougoutas,Hedberg,Kimball,Malley,Moreland,Porubcan,Pudzianowski
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p. 936 - 944
(2007/10/02)
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