- NURR1 RECEPTOR MODULATORS
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Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.
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Paragraph 0646; 1213-1215
(2020/09/08)
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- Preparation of Organic Nitrates from Aryldiazoacetates and Fe(NO3)3·9H2O
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A thermal protocol is reported for the formal insertion of nitric acid into aryldiazoacetates using Fe(NO3)3·9H2O. This strategy is mild and high yielding and allows the preparation of a large variety of members of an unprecedented family of organic nitrates. The nitrate group can be also readily transformed into other functional groups and heterocyclic moieties and can possibly allow new biological explorations of untapped potential associated with their NO-releasing ability.
- Thurow, Samuel,Fernandes, Alessandra A. G.,Quevedo-Acosta, Yovanny,De Oliveira, Matheus F.,De Oliveira, Marcelo G.,Jurberg, Igor D.
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p. 6909 - 6913
(2019/09/12)
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- Rapid Assembly of Saturated Nitrogen Heterocycles in One-Pot: Diazo-Heterocycle “Stitching” by N–H Insertion and Cyclization
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Methods that provide rapid access to new heterocyclic structures in biologically relevant chemical space provide important opportunities in drug discovery. Here, a strategy is described for the preparation of 2,2-disubstituted azetidines, pyrrolidines, pi
- Boddy, Alexander J.,Affron, Dominic P.,Cordier, Christopher J.,Rivers, Emma L.,Spivey, Alan C.,Bull, James A.
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supporting information
p. 1458 - 1462
(2019/01/04)
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- Efficient microwave-assisted esterification reaction employing methanesulfonic acid supported on alumina as catalyst
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A rapid and efficient protocol assisted by microwave irradiation for the synthesis of esters using methanesulfonic acid (CH3SO3H) supported on Al2O3 (AMA) as catalyst and free of solvent is described. The products were obtained in good yields and purity, with reduced reaction time, and the process is simple and environmentally benign. Copyright
- Fabian, Lucas,Gomez, Matias,Kuran, Juan A. Caturelli,Moltrasio, Graciela,Moglioni, Albertina
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p. 2386 - 2392
(2014/07/22)
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- Nature and kinetic analysis of carbon-carbon bond fragmentation reactions of cation radicals derived from SET-oxidation of lignin model compounds
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Features of the oxidative cleavage reactions of diastereomers of dimeric lignin model compounds, which are models of the major types of structural units found in the lignin backbone, were examined. Cation radicals of these substances were generated by using SET-sensitized photochemical and Ce(IV) and lignin peroxidase promoted oxidative processes, and the nature and kinetics of their C- bond cleavage reactions were determined. The results show that significant differences exist between the rates of cation radical C1-2 bond cleavage reactions of 1,2-diaryl-(β-1) and 1-aryl-2-aryloxy-(β-O-4) propan-1,3-diol structural units found in lignins. Specifically, under all conditions C1-2 bond cleavage reactions of cation radicals of the β-1 models take place more rapidly than those of the β-O-4 counterparts. The results of DFT calculations on cation radicals of the model compounds show that the C1-2 bond dissociation energies of the β-1 lignin model compounds are significantly lower than those of the β-O-4 models, providing clear evidence for the source of the rate differences.
- Cho, Dae Won,Parthasarathi, Ramakrishnan,Pimentel, Adam S.,Maestas, Gabriel D.,Park, Hea Jung,Yoon, Ung Chan,Dunaway-Mariano, Debra,Gnanakaran,Langan, Paul,Mariano, Patrick S.
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supporting information; experimental part
p. 6549 - 6562
(2010/12/19)
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- Enzymatic desymmetrization of prochiral 2-substituted-1,3-diamines: Preparation of valuable nitrogenated compounds
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A wide range of prochiral 1, 3-diamines were first efficiently synthesized and subsequently desymmetrized by using lipase from Pseudomonas cepacia as catalyst and diallyl carbonate as alkoxycarbonylating agent. In all cases, the amino carbamates of R-configuration were recovered. Final selective cleavage of the N-allyloxycarbonyl moiety was carried out under mild reaction conditions, which demonstrates the high versatility and potential of this chemoenzymatic route as a source of intermediates in the synthesis of related optically active nitrogenated derivatives.
- Rios-Lombardia, Nicolas,Busto, Eduardo,Garcia-Urdiales, Eduardo,Gotor-Fernandez, Vicente,Gotor, Vicente
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supporting information; experimental part
p. 2571 - 2574
(2009/07/25)
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- 4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors
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A series of non-nucleoside adenosine kinase (AK) inhibitors is reported. These inhibitors originated from the modification of 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine (ABT-702). The identification of a linker that would approximate the spatial arrangement found between the pyrimidine ring and the aryl group at C(7) in ABT-702 was a key element in this modification. A search of potential linkers led to the discovery of an acetylene moiety as a suitable scaffold. It was hypothesized that the aryl acetylenes, ABT-702, and adenosine bound to the active site of AK (closed form) in a similar manner with respect to the orientation of the heterocyclic base. Although potent acetylene analogs were discovered based on this assumption, an X-ray crystal structure of 5-(4-dimethylaminophenyl)-6-(6-morpholin-4-ylpyridin-3-ylethynyl)pyrimidin-4-ylamine (16a) revealed a binding orientation contrary to adenosine. In addition, this compound bound tightly to a unique open conformation of AK. The structure-activity relationships and unique ligand orientation and protein conformation are discussed.
- Matulenko, Mark A.,Paight, Ernest S.,Frey, Robin R.,Gomtsyan, Arthur,DiDomenico Jr., Stanley,Jiang, Meiqun,Lee, Chih-Hung,Stewart, Andrew O.,Yu, Haixia,Kohlhaas, Kathy L.,Alexander, Karen M.,McGaraughty, Steve,Mikusa, Joseph,Marsh, Kennan C.,Muchmore, Steven W.,Jakob, Clarissa L.,Kowaluk, Elizabeth A.,Jarvis, Michael F.,Bhagwat, Shripad S.
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p. 1586 - 1605
(2008/02/01)
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- Design of polyaromatic hydrocarbon-supported tin reagents: A new family of tin reagents easily removable from reaction mixtures
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We report in this paper the preparation and use of stannanes 11, 12a, and 12b, compounds whose 3-pyrenylpropyl side chain affinity for activated carbon simplifies tin removal and product isolation. Our pyrene-supported reagents can be used for radical reductions and cyclizations (11), radical and cationic allylations (12a), and Stille couplings (12b) in much the same way as tributyltin derivatives.
- Stien, Didier,Gastaldi, Stephane
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p. 4464 - 4470
(2007/10/03)
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- A highly convenient, efficient, and selective process for preparation of esters and amides from carboxylic acids using Fe3+-K-10 montmorillonite clay
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In the presence of Fe3+-K-10 montmorillonite clay as a catalyst, aliphatic carboxylic acids selectively produced the corresponding esters in the presence of aromatic carboxylic acids by treatment with alcohols. Both the aliphatic and aromatic carboxylic acids formed the amides by reacting with the aliphatic amines, but only the aliphatic carboxylic acids yielded the anilides by treatment with aromatic amines. The catalyst is recoverable and recyclable.
- Srinivas,Das, Biswanath
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p. 1165 - 1167
(2007/10/03)
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- 1,2-disubstituted-6-oxo-3-phenyl-piperidine-3-carboxamides and combinatorial libraries thereof
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The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
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- PAH-supported tin hydride: A new tin reagent easily removable from reaction mixtures
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We demonstrate here that a new pyrene-supported tin hydride can be used in radical chemistry. Final products were easily purified by adsorption of the PAH-supported tin side product with activated carbon.
- Gastaldi, Stéphane,Stien, Didier
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p. 4309 - 4311
(2007/10/03)
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- On a baker's yeast-mediated approach to verapamil's optically active intermediates
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Racemic hydroxylactones 11a and 11b were converted through the key aldehyde intermediate 21 into the C6-C4 acid 22, showing all the necessary functionalities for the subsequent transformation into verapamil 1. Baker's yeast reduction
- Brenna, Elisabetta,Caraccia, Nicola,Fogliato, Giovanni,Fronza, Giovanni,Fuganti, Claudio
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p. 10555 - 10564
(2007/10/03)
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- Unexpected alkylation reaction of amines, acids and phenols by alkyl (triphenylphosphoranylidene)acetates
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Reaction of methyl (triphenylphosphoranylidene)acetate in methanol with primary and secondary amines led to N-methylated derivatives. Similarly this mixture reacted with acids, phenol and phthalimide to afford methyl esters, anisole and N-methylphthalimide respectively. Treatment of ketolactam 2 by this mixture under high pressure activation gave the rearranged quinolinone 5.
- Desmaele, Didier
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p. 1233 - 1236
(2007/10/03)
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- ELECTRFLUORATION EN POSITION BENZYLIQUE DANS LE SULFOLANE
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The use of sulfolane as a solvent instead of acetonitrile in the electrofluorination of benzylic derivatives 1, (R=H, Cl) gives greater yields of benzylic fluorides 2, since the formation of acetamide byproducts 4 is prevented.However, the parallel fluorination of the aromatic nucleus is not avoided under these conditions.
- Laurent, Eliane,Marquet, Bernard,Tardivel, Robert
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p. 115 - 126
(2007/10/02)
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- BENZOPHENANTHRIDINES V. INVESTIGATION OF THE RODIONOV-SUVOROV SCHEME. SYNTHESIS OF 3,3-DIETHOXYCARBONYL-2-(3,4-DIMETHOXYPHENYL)-6,7-DIMETHOXY-1-TETRALONE
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Triethyl 1,3-bis(3,4-dimethoxyphenyl)propane-1,2,2-tricarboxylate was synthesized by the alkylation of the lithium enolate of ethyl homoveratrate with α-bromo(3,4-dimethoxybenzyl)malonic ester.It was converted by intramolecular acylation, catalyzed by BF3
- Kyong, Dao Hung,Sladkov, V. I.,Suvorov, N. N.
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p. 1732 - 1738
(2007/10/02)
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