José F. Soriano

CCDC 1820730: Experimental Crystal Structure Determination

Ana B. Bueno, Javier Agejas, Howard B. Broughton, Robert Dally et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Optimization of Hydroxyethylamine Transition State Isosteres as Aspartic Protease Inhibitors by Exploiting Conformational Preferences

Ana B. Bueno, Javier Agejas, Howard B. Broughton, Robert Dally et autres

NMR conformational analysis of a hydroxyethylamine peptide isostere developed as an aspartic protease inhibitor shows that it is a flexible architecture. Cyclization to form pyrrolidines, piperidines, or morpholines results in a preorganization of the whole system in solution. The resulting conformation is …

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Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity

Mark D. Chappell, Renhua Li, Stephon C. Smith, Bruce A. Dressman et autres

As part of our ongoing efforts to identify novel ligands for the metabotropic glutamate 2 and 3 (mGlu 2/3 ) receptors, we have incorporated substitution at the C3 and C4 positions of the (1 S,2 R,5 R,6 R )-2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid scaffold to …

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Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression

Bruce A. Dressman, Eric G. Tromiczak, Mark D. Chappell, Allie E. Tripp et autres

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Metabotropic Glutamate Receptor in complex with antagonist (1~{S},2~{R},3~{S},4~{S},5~{R},6~{R})-2-azanyl-3-[[3,4-bis(fluoranyl)phenyl]sulfanylmethyl]-4-oxidanyl-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid

Mark D. Chappell, R. Li, Stephon C. Smith, Bruce A. Dressman et autres

Perceived Vulnerability to Disease Questionnaire: Factor structure, psychometric properties and gender differences

Amelia Díaz, José F. Soriano, Ángela Beleña

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Perceived Vulnerability to Disease Questionnaire--Spanish Version

Amelia Díaz, José F. Soriano, Ángela Beleña

Regio- and stereoselective synthesis of pyrrolo or azepine-fused cyclopenta[d]isoxazolines from 2-p-tolylsulfinylcyclopent-2-en-1-one

J.L.G. Ruano, José F. Soriano, Alberto Fraile, Michel Martin et autres

Reactions of enantiopure 2-p-tolylsulfinylcyclopent-2-en-1-one with cyclic nitrones afforded pyrrolo or azepine-fused cyclopenta[d]isoxazolidines in high yields under mild conditions. Comparison of these results with those obtained with cyclopent-2-en-1-one as the dipolarophile shows that the sulfinyl group increases the reactivity of the enonic system …

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O-(Mesitylsulfonyl)hydroxylamine

Gernot Boche, Javier Mendiola, Juan A. Rincón, Carlos Mateos et autres

[36016-40-7] C9H13NO3S (MW 215.2) InChI = 1S/C9H13NO3S/c1-6-4-7(2)9(8(3)5-6)14(11,12)13-10/h4-5H,10H2,1-3H3 InChIKey = CHKQALUEEULCPZ-UHFFFAOYSA-N (reagent for electrophilic aminations, NH2 transfer to nucleophiles) Physical Date: mp 93–94 °C.1 Solubility: very sol diethyl ether, chloroform, dichloromethane, benzene, ethanol, THF; insol water and petroleum ether. Analysis of Reagent Purity: …

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Synthesis of condensed isoxazolines and isoxazolidines via cycloaddition to furan-2(5H)-ones

J.L.G. Ruano, Cristina Fajardo, Alberto Fraile, Michel Martin et autres

Cycloadditions of nitrone 1 and pyridylnitrile oxide 4 to furanones 2 and 3 afford tetrahydrofuro[3',4':4,5]isoxazolo[2,3-a]dibenzo[c,f]azepin-1(3H)-ones and furo[3,4d]isoxazolin-4(H)-ones, respectively, in a totally regioselective manner.The resulting adducts evolve into the corresponding pyrroloisoxazole systems by treatment with ammonium hydroxide and hydrazine hydrate in good yield.The …

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Preparation, Use, and Safety of O-Mesitylenesulfonylhydroxylamine

Javier Mendiola, Juan A. Rincón, Carlos Mateos, José F. Soriano et autres

The aminating reagent O -mesitylsulfonylhydroxylamine (MSH) has a known potential hazard since it contains high-energy functional groups in its structure. There are references in the literature that report several incidents involving the use of pure and crystalline MSH. The preparation and safe …

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Synthesis of a Novel Series of 4,4‐Disubstituted 2,3,4,7‐Tetrahydroazepines.

Mario Barberis, Pablo García‐Losada, Sehila Pleite, Ramón Rodríguez et autres

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