End-to-End Automated Synthesis of C(sp3)-Enriched Drug-like Molecules via Negishi Coupling and Novel, Automated Liquid-Liquid Extraction.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01646
Abstract: Herein, we report an end-to-end process including synthesis, work-up, purification, and post-purification with minimal human intervention using Negishi coupling as a key transformation to increase Fsp3 in bioactive molecules. The main advantages of this protocol… read more here.
Keywords: end end; liquid liquid; liquid; end ... See more keywords
Synthesis of Electron-Deficient Heteroaromatic 1,3-Substituted Cyclobutyls via Zinc Insertion/Negishi Coupling Sequence under Batch and Automated Flow Conditions.
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DOI: 10.1021/acs.orglett.8b03588
Abstract: Synthesis of 1,3-substituted cyclobutyls enabled by zinc insertion into functionalized iodocyclobutyl derivatives followed by Negishi coupling with halo-heteroaromatics is reported. Two distinct sets of conditions were developed; the first involved a two-step batch protocol using… read more here.
Keywords: substituted cyclobutyls; zinc insertion; synthesis electron; negishi coupling ... See more keywords
Model Compounds for Intermediates and Transition States in Sonogashira and Negishi Coupling: d8-d10 Bonds in Large Heterobimetallic Complexes Are Weaker than Computational Chemistry Predicts.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.2c01641
Abstract: We report an experimental study, with accompanying DFT calculations, on a series of heterobimetallic complexes with Pd(II) and Cu(I), Ag(I), or Au(I). The isolable pincer complexes are models for the intermediates and transition state for… read more here.
Keywords: heterobimetallic complexes; chemistry; sonogashira negishi; negishi coupling ... See more keywords