- Hydroboration reduction reaction of aromatic nitro compounds without transition metal catalysis
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The invention relates to a hydroboration reduction reaction of aromatic nitro compounds without transition metal catalysis. According to the method, triethyl boron and potassium tert-butoxide are used as catalysts for the first time, and an aromatic nitro compound and pinacol borane which is low in price and easy to obtain can be conveniently catalyzed to be subjected to a hydroboration reduction reaction under mild conditions to prepare aromatic amine products. Compared with a traditional method, the method generally has the advantages that the catalyst is cheap and easy to obtain, operation is convenient, and reaction is safe. The selective hydroboration reduction reaction of the non-transition metal reagent catalyzed aromatic nitro compound and pinacol borane is realized for the first time, and a practical new reaction strategy is provided for laboratory preparation or industrial production of aromatic amine products.
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Paragraph 0006; 0069-0072
(2021/07/31)
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- Innovative Multipodal Ligands Derived from Tr?ger's Bases for the Sensitization of Lanthanide(III) Luminescence
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Herein, the synthesis and characterization of the first family of multipodal ligands with a Tr?ger's base framework designed for the preparation of luminescent lanthanide(III) complexes are reported. Eight ligands were designed and synthesized using diffe
- Barja, Beatriz C.,Bruttomesso, Andrea C.,Eliseeva, Svetlana V.,Petoud, Stéphane,Ramírez, Javier A.,Trupp, Leandro,Vardé, Mariana
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p. 16900 - 16909
(2020/11/30)
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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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- Carbonyl Iron Powder: A Reagent for Nitro Group Reductions under Aqueous Micellar Catalysis Conditions
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An especially mild, safe, efficient, and environmentally responsible reduction of aromatic and heteroaromatic nitro-group-containing educts is reported that utilizes very inexpensive carbonyl iron powder (CIP), a highly active commercial grade of iron powder. These reductions are conducted in the presence of nanomicelles composed of TPGS-750-M in water, a recyclable aqueous micellar reaction medium. This new technology also shows broad scope and scalability and presents opportunities for multistep one-pot sequences involving this reducing agent.
- Lee, Nicholas R.,Bikovtseva, Agata A.,Cortes-Clerget, Margery,Gallou, Fabrice,Lipshutz, Bruce H.
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supporting information
p. 6518 - 6521
(2017/12/26)
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- SULFONAMIDE COMPOUNDS AND THEIR USE AS STAT5 INHIBITORS
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The present disclosure relates to compounds having the Formula (Formula (I)) which are inhibitors of STAT5.
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Paragraph 00160; 00171-00172
(2015/12/17)
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- Chemoselective N-deacetylation under mild conditions
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A mild and efficient chemoselective N-deacetylation using the Schwartz reagent at room temperature in rapid time is described. The mild and neutral conditions enable orthogonal N-deacetylation in the presence of some of the common protecting groups (viz. Boc, Fmoc, Cbz, Ts). The deprotection conditions did not induce any epimerization at the chiral amino centre.
- Sultane, Prakash R.,Mete, Trimbak B.,Bhat, Ramakrishna G.
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supporting information
p. 261 - 264
(2014/01/06)
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- Preparation of functionalized indoles and azaindoles by the intramolecular copper-mediated carbomagnesiation of ynamides
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Variations on a theme: A mild and general intramolecular copper-mediated carbomagnesiation procedure for the synthesis of functionalized indoles as well as 4-, 5-, 6-, and 7-azaindoles starts from readily available ynamides. Subsequent reactions with various electrophiles provides polyfunctional N-heterocycles in good yields.
- Frischmuth, Annette,Knochel, Paul
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supporting information
p. 10084 - 10088
(2013/10/01)
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- MATRIX METALLOPROTEINASE INHIBITORS
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The present invention relates to methyl sulfonamides and N-formamides derivatives of formula (I) and to processes for their syntheses. The invention also relates to pharmacological compositions containing these derivatives and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatie arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation which leads to restenosis and ischemic heart failure, stroke, renal disease, tumor metastasis, and other inflammatory disorders characterized by over expression and over activation of an matrix metalloproteinase using the compounds.
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- Carbamic acid 2-trimethylsilylethyl ester as a new ammonia equivalent for palladium-catalyzed amination of aryl halides
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Carbamic acid 2-trimethylsilylethyl ester (Teoc-NH2) serves as an ammonia equivalent in the palladium-catalyzed amination of aryl bromides and aryl chlorides. Anilines with sensitive functional groups can be readily prepared using these amine derivatives.
- Mullick, Dibakar,Anjanappa, Prakash,Selvakumar, Kumaravel,Ruckmani, Kandasamy,Sivakumar, Manickam
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supporting information; experimental part
p. 5984 - 5987
(2010/11/21)
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- TARGETING PRODRUGS AND COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES
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Provided herein are compounds, compositions and methods for preventing or treating gastrointestinal cancer in a mammal, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulfonamide inhibitor as a prodrug or derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in- vivo.
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Page/Page column 30-31
(2010/07/09)
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- UREYLENE DERIVATIVES
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The invention concerns compounds of Formula (I) or a salt, solvate or pro-drug thereof. The compounds may be used in therapy, particularly anti-cancer therapy.
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- Rational design of substituted diarylureas: A scaffold for binding to G-quadruplex motifs
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The design and synthesis of a series of urea-based nonpolycyclic aromatic ligands with alkylaminoanilino side chains as telomeric and genomic G-quadruplex DNA interacting agents are described. Their interactions with quadruplexes have been examined by means of fluorescent resonance energy transfer melting, circular dichroism, and surface plasmon resonance-based assays. These validate the design concept for such urea-based ligands and also show that they have significant selectivity over duplex DNA, as well as for particular G-quadruplexes. The ligand-quadruplex complexes were investigated by computational molecular modeling, providing further information on structure-activity relationships. Preliminary biological studies using short-term cell growth inhibition assays show that some of the ligands have cancer cell selectivity, although they appear to have low potency for intracellular telomeric G-quadruplex structures, suggesting that their cellular targets may be other, possibly oncogene-related quadruplexes.
- Drewe, William C.,Nanjunda, Rupesh,Gunaratnam, Mekala,Beltran, Monica,Parkinson, Gary N.,Reszka, Anthony P.,Wilson, W. David,Neidle, Stephen
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supporting information; experimental part
p. 7751 - 7767
(2009/12/07)
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- Synthesis, structure-activity relationship, and p210bcr-abl protein tyrosine kinase activity of novel AG 957 analogs
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A series of novel, sterically hindered lipophilic analogs of AG 957 was designed and synthesized as potential protein tyrosine kinase (PTK) inhibitors. The in vitro activity, in vivo anti-leukemia activity, and pharmacology of these PTK inhibitors were studied. Some aspects of the structure-activity relationship associated with the carboxylic acid, phenol ring, and linker modifications are discussed. We have demonstrated that the 1,4-hydroquinone moiety is essential for activity and that sterically hindered esters contribute to enhanced in vivo efficacy. Adaphostin (NSC 680410) has emerged as the improved compound with the maximum in vivo anti-leukemia hollow fiber activity, concordant with the original lead compound AG 957. Currently, adaphostin is undergoing preclinical toxicology studies.
- Kaur, Gurmeet,Narayanan, Ven L.,Risbood, Prabhakar A.,Hollingshead, Melinda G.,Stinson, Sherman F.,Varma, Ravi K.,Sausville, Edward A.
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p. 1749 - 1761
(2007/10/03)
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- New selenyl linker for solid-phase synthesis of dehydropeptides
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A novel linker possessing selenocyanate and masked carboxylic acid was developed for the solid-phase synthesis of dehydropeptides. This linker was used to demonstrate the synthesis of the model compound of RGD-conjugated dehydropeptide.
- Nakamura, Kazuhiko,Ohnishi, Yuki,Horikawa, Eiji,Konakahara, Takeo,Kodaka, Masato,Okuno, Hiroaki
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p. 5445 - 5448
(2007/10/03)
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- Disubstituted lavendustin a analogs and pharmaceutical compositions comprising the analogs
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Disubstituted lavendustin A analogs that are PTK inhibitors having antiproliferative activity are described. Preferred compounds of the present invention, without limitation, satisfy either Formula 1 or Formula 2. Currently preferred compounds ,based on in vivo biological activity, are 4'-adamantylbenzoate-1'-N-1,4-dihydroxybenzylamine and 4'-adamantylmethylbenzoate-1'-N-1,4-dihydroxybenzylamine. The present invention also provides pharmaceutical compositions comprising effective amounts of disubstituted lavendustin A analogs. Such compositions also may comprise other active ingredients, other materials conventionally used in the formulation of pharmaceutical composition, and mixtures thereof. The compounds and compositions of the present invention can be used for treating subjects to, for example, inhibit the proliferation of living cells in the treatment of proliferative diseases.
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- Palladium-Catalyzed Animation of Aryl Halides on Solid Support
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(Matrix Presented) The first examples of the Pd(0)-catalyzed amination of aryl halides using Rink-resins as nitrogen source are described. Pd2dba3/BINAP/NaO-t-Bu was found to be the most efficient catalyst/base system, while a solvent mixture of dioxane and tert-butyl alcohol was shown to enhance the selectivity toward the desired monoarylation. Moderate to good yields and excellent purities of the amination products were found with electron-poor aryl halides, while electon-rich aryl halides failed to react under these conditions.
- Weigand, Klaus,Pelka, Sylvie
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p. 4689 - 4692
(2007/10/03)
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- Template-constrained cyclic peptide analogues of somatostatin: Subtype-selective binding to somatostatin receptors and antiangiogenic activity
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β-Turns are a common secondary structure motif found in proteins that play a role in protein folding and stability and participate in molecular recognition interactions. Somatostatin, a peptide hormone possessing a variety of therapeutically-interesting b
- Suich, Daniel J.,Mousa, Shaker A.,Singh, Gurke,Liapakis, George,Reisine, Terry,Degrado, William F.
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p. 2229 - 2241
(2007/10/03)
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- α,α-difluorophosphonomethyl azobenzene derivatives as photoregulated phosphoamino acid analogs. 1. Design and synthesis
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A series of novel, photoregulated phosphoamino acid analogs based on an azobenzene core bearing an α,α-difluoromethylphosphonate as a hydrolytically stable phosphate isostere have been prepared with N-Fmoc protection for use in peptide synthesis. Classes of reagents analogous to both phosphotyrosine and phosphoserine/threonine were prepared by a common route employing a nitrosoarene/aniline condensation to form the azo linkage and the Cu(I)-promoted coupling of an iodoarene with (diethylphosphono)difluoromethyl cadmium bromide (Burton's method) to introduce the phosphonate moiety.
- Park, Seung Bum,Standaert, Robert F.
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p. 6557 - 6560
(2007/10/03)
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- Liquid-Phase Hydrogenation of p-Nitrobenzoic Acid Esters on Palladium Catalysts
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Hydrogenation of some p-nitrobenzoic esters on palladium catalysts (conventional heterogeneous Pd/C and Pd/Al2O3 and polymeric AV-17-8-Pd and AN-1-Pd) is studied. The maximum rate of the hydrogenation reaction was observed in methanol at t = 55°C and PH2 = 0.1 MPa. MNDO calculations of some electronic characteristics of p-nitrobenzoic ester molecules were performed. A two-parameter correlation between the hydrogenation rate constant, the charge of the nitro group, and the steric substituent constant was found for the reaction conducted on the AV-17-8-Pd and AN-1-Pd catalysts.
- Morogina,Nasibulin,Klyuev
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p. 251 - 255
(2007/10/03)
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- Change of the Rate-Determining Stage in the Hydrogenation of Nitrobenzene. Effect of Solvent and Catalyst
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The rate-determining stage in the hydrogenation of nitrobenzene in ethanol over palladium-containing flexible polymers or Pd/C is reduction of the nitro group to nitroso. In 2-propanol, the rate-determining stage is reduction of the nitroso group. When the hydrogenation is performed over palladium-containing hard polymers, change of the solvent does not result in change of the rale-determining stage which is reduction of the nitroso group.
- Voronin,Nasibulin,Klyuev
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p. 1613 - 1615
(2007/10/03)
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- Quinazoline antifolate thymidylate synthase inhibitors: Replacement of glutamic acid in the C2-methyl series
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The synthesis of a series of analogues of the potent thymidylate synthase (TS) inhibitor N-[4[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N- prop-2-ynylamino]benzoyl]-L-glutamic acid (ICI 198583, 1) is described in which the glutamic acid residu
- Marsham,Jackman,Barker,Boyle,Pegg,Wardleworth,Kimbell,O'Connor,Calvert,Hughes
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p. 994 - 1004
(2007/10/02)
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- Novel enzyme derivatives
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A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.
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- A CONVENIENT SYNTHESIS OF t-BUTYL p-AMINOBENZOATE
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A convenient one-pot synthesis of t-butyl p-aminobenzoate is described which involves treatment of p-aminobenzoic acid with thionyl chloride, followed by reaction of the resulting p-sulfinylaminobenzoyl chloride with t-butanol.
- Taylor, Edward C.,Fletcher, Stephen R.,Sabb, Annmarie L.
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p. 921 - 924
(2007/10/02)
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