Anionic Amino-Cope Rearrangement Cascade Synthesis of 2,4-Substituted Benzoate Esters from Acyclic Building Blocks

Review Chemistry, Multidisciplinary

Recent Developments for the Deuterium and Tritium Labeling of Organic Molecules

Sara Kopf et al.

Summary: Organic compounds labeled with hydrogen isotopes are crucial in drug discovery and development in the pharmaceutical industry. Recent advancements have been made in methodologies for isotopic enrichment of organic molecules, including hydrogen isotope exchange reactions, isotopically labeled analogues of organic reagents, and other transformations with isotope incorporation.

CHEMICAL REVIEWS (2022)

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Article Chemistry, Applied

Development of a Commercial Process for Deucravacitinib, a Deuterated API for TYK2 Inhibition

Daniel S. Treitler et al.

Summary: Deucravacitinib is a deuterated small-molecule TYK2 inhibitor developed for the treatment of autoimmune disorders. The development of a new synthesis route and impurity control allowed for large-scale production of Deucravacitinib for clinical and commercial use.

ORGANIC PROCESS RESEARCH & DEVELOPMENT (2022)

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Article Chemistry, Multidisciplinary

Dramatic Effect of γ-Heteroatom Dienolate Substituents on Counterion Assisted Asymmetric Anionic Amino-Cope Reaction Cascades

Pradipta Das et al.

Summary: This study reveals the significant impact of different gamma-dienolate heteroatom substituents on the product outcomes of lithium ion enabled amino-Cope-like anionic asymmetric cascade reactions. Depending on the substituents, the reaction pathways vary, leading to different relationships between stereocenters in the resulting products. The presence of a lithium counterion is found to be essential in these reactions, which are solvent- and counterion-dependent.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Article Chemistry, Organic

Dienolate Annulation Approach for Assembly of Densely Substituted Aromatic Architectures

Kevin A. Scott et al.

Summary: This study presents an efficient method for assembling complex aromatic structures from simple acyclic building blocks by anion-cascade union of an enoate and a conjugated imine. The intermediate cyclohexenones are further transformed into chiral cyclohexadienes and diverse aromatic architectures through Grignard reagents and enol triflates, respectively.

JOURNAL OF ORGANIC CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary