Talbi Kaoudi

CCDC 2408183: Experimental Crystal Structure Determination

Thomas J. Beauchamp, Kevin P. Cole, Howard B. Broughton, David A. Coates 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, …

Preclinical Toxicology Supply for a Complex API Enabled by Asymmetric Catalysis and Rapid Chemical Development: IL-17A Inhibitor LY3509754

Thomas J. Beauchamp, Kevin P. Cole, Howard B. Broughton, David A. Coates et autres

The chemical development and production of sufficient amounts of IL-17A inhibitor LY3509754 to enable preclinical toxicology studies is described. LY3509754 is a complex small molecule that features three stereocenters, which comprised much of the synthetic challenge. Stereoselective hydrogenation and biocatalysis enabled access …

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Synthesis, Optimization, and Large-Scale Preparation of the Low-Dose Central Nervous System-Penetrant BACE1 Inhibitor LY3202626 via a [3 + 2] Nitrone Cycloaddition

Pablo García‐Losada, Amy C. DeBaillie, José Eugenio de Diego, Steven J. Green et autres

Herein we report a summary of the synthetic development of LY3202626 from the initial discovery route to a final route that was scaled to make 150 kg. Key developments include the use of a [3 + 2] cyclization to set the cis …

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Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor

Huaxing Pei, Saravanan Parthasarathy, Sajan Joseph, William T. McMillen et autres

Abstract The transforming growth factor β (TGFβ) signaling pathway is a pleiotropic cellular pathway that plays a critical role in cancer. In fact, aggressive tumors are typically associated with high ligand levels and thus associated with poor prognosis in various tumor types. …

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Enantioselective Synthesis of 3,3-Difluoropyrrolidin-4-ol, a Valuable Building Block in Medicinal Chemistry

Chong Si, Kevin R. Fales, Alicia Torrado, Kwame Frimpong et autres

In this paper, we report for the first time two enantioselective routes to 4,4-difluoropyrrolidin-3-ol, a valuable building block in medicinal chemistry. In the first route, we took advantage of the C2 symmetry of (3R,4R)-3,4-dihydroxypyrrolidine in which the desired chirality was derived from …

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CCDC 282661: Experimental Crystal Structure Determination

Imad Safir, Isabel Castellote, Susana Porcel, Talbi Kaoudi 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, …

CCDC 282660: Experimental Crystal Structure Determination

Imad Safir, Isabel Castellote, Susana Porcel, Talbi Kaoudi 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, …

CCDC 282662: Experimental Crystal Structure Determination

Imad Safir, Isabel Castellote, Susana Porcel, Talbi Kaoudi 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, …

CCDC 610968: Experimental Crystal Structure Determination

Laure Finet, Mohamed Dakir, Isabel Castellote, Talbi Kaoudi 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, …

CCDC 611342: Experimental Crystal Structure Determination

Laure Finet, Mohamed Dakir, Isabel Castellote, Talbi Kaoudi 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, …

Synthesis of Chiral Ligands from Hydrindene Diols with a Consecutive Heterodomino Transformation as the Key Reaction Step

Laure Finet, Mohamed Dakir, Isabel Castellote, Talbi Kaoudi et autres

Abstract We report here the elaboration of a bicyclo[2.2.2]octane system, synthesized by a consecutive domino process, towards highly functionalized stereopure derivatives, which could be used as multidentate ligands for the generation of asymmetric catalysts. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 …

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Rate constants for 1,n-hydrogen transfer reactions in some amino acid derived radicals

Le Zeng, Talbi Kaoudi, Carl H. Schiesser

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