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Diversity‐Oriented Synthesis of Morpholine‐Containing Molecular Scaffolds
Chemistry – A European Journal, 2009Couple and cyclize: A coupling–cyclization strategy employing building blocks from the chiral pool was applied for the generation of morpholine-containing scaffolds (see scheme). The modulation of both the reaction conditions and the stereochemistry of the building blocks allowed the first degree of skeletal diversity, followed by functional group ...
LALLI, CLAUDIA +4 more
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Diversity-Oriented Synthesis of Bioactive Azaspirocycles
Tetrahedron, 2019Abstract A collection of novel azaspirocyclic β-arylethylamines was prepared in good yield and excellent diastereoselectivity by an expedient strategy that features condensation of a cyclic ketone with an amino allylsilane and a tandem aza-Sakurai cyclization to generate several different spirocyclic N-heterocycles.
Lance T. Lepovitz, Stephen F. Martin
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Diversity Oriented Synthesis: A Challenge for Synthetic Chemists
2006This article covers the diversity-oriented synthesis (DOS) of small molecules in order to generate a collection of pure compounds that are attractive for lead generation in a phenotypic, high-throughput screening approach useful for chemical genetics and drug discovery programmes.
A, Bender +10 more
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ChemInform Abstract: Diversity‐Oriented Synthesis
ChemInform, 2009AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Richard J. Spandl +4 more
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2013
Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways.
TRABOCCHI, ANDREA +36 more
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Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways.
TRABOCCHI, ANDREA +36 more
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Diversity‐Oriented Synthesis of Calothrixins and Ellipticines
European Journal of Organic Chemistry, 2014AbstractThe divergent synthesis of calothrixins and ellipticines has been accomplished by utilising the one‐pot formation of o‐diacylarenes as a key intermediate through rearrangement of o‐hydroxy ketone monoacyl hydrazones by lead tetraacetate mediated oxidation.
Dattatraya H. Dethe, Ganesh M. Murhade
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Diversity oriented synthesis of benzoxazoles and benzothiazoles
Tetrahedron Letters, 2007Abstract A combinatorial synthetic route yielding benzoxazoles and benzothiazoles is described. The use of o -halophenylisocyanides in the Ugi reaction (U-4CR) followed by a copper-catalyzed cyclization affords the benzoxazole as well as the benzothiazole moiety in good yield and high diversity.
Julia H. Spatz +6 more
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The diversity‐oriented synthesis of pteridines—achievements and potential for development
IUBMB Life, 2013AbstractThe importance of pteridines in the key cofactors, tetrahydrofolate and tetrahydrobiopterin, has encouraged the development of the chemistry and chemical biology of pteridines. In order to investigate the latter, versatile synthetic methods are required to prepare designed relatives of the natural cofactors for use as potential drugs or ...
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Structural diversity-oriented synthesis
The DMP is focused on exploration of skeletal transformations of beta-caryophyllene, one of most accessible sesquiterpenes. This abundant natural product possesses cyclobutane and E-cyclononene fragments, which have an intrinsic aptitude to form other scaffolds under various reaction conditions.openaire +2 more sources
Some Principles of Diversity-Oriented Synthesis
2011Chemical genetics has recently established itself as a systematic and powerful tool for exploring the biological world by exploiting the structural diversity of small molecules, notably with the aim of probing proteins (see chapter 2). Inhibiting the activity of a protein with a small molecule (a ligand) corresponds to eliminating the gene with which ...
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