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Synthesis of Privileged Scaffolds by Using Diversity‐Oriented Synthesis
Chemistry – An Asian Journal, 2013AbstractAn elegant reagent‐controlled strategy has been developed for the generation of a diverse range of biologically active scaffolds from a chiral bicyclic lactam. Reduction of the chiral lactam with LAH or alkylation with LHMDS to trigger different cyclization reactions have been shown to generate privileged scaffolds, such as pyrrolidines ...
Ramu, Surakanti +9 more
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Diversity-oriented synthesis; a spectrum of approaches and results
Organic & Biomolecular Chemistry, 2008Since our emerging area article, diversity-oriented synthesis (DOS), which aims to prepare efficiently collections of skeletally diverse small molecules, has developed in the synthetic approaches it employs. This article describes three general strategies, highlighting some successful examples. The utility of DOS, in the interrogation of chemical space
Richard J, Spandl +2 more
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Enriching Chemical Space with Diversity‐Oriented Synthesis
ChemInform, 2007AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Gemma L, Thomas +2 more
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Diversity-Oriented Synthesis of Polycyclic Diazinic Scaffolds
Organic Letters, 2012An efficient and versatile synthesis of a polycyclic diazinic system starting from oxazine has been developed using a two-step Michael/retro Michael and cyclization sequence. The substrates were synthesized with good to high yields giving rapid access to molecular diversity.
Nicolas, Gigant +3 more
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Diversity-oriented synthesis of bicyclic and tricyclic alkaloids
Chem. Commun., 2010A diversity-oriented synthesis involving a cascade sequence, taking linear aminoalkenes to polycyclic scaffolds reminiscent of natural alkaloids, is presented.
Mónica, Díaz-Gavilán +4 more
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Furans as versatile synthons for target-oriented and diversity-oriented synthesis
ChemInform, 2005AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
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Target-Oriented and Diversity-Oriented Organic Synthesis in Drug Discovery
Science, 2000Modern drug discovery often involves screening small molecules for their ability to bind to a preselected protein target. Target-oriented syntheses of these small molecules, individually or as collections (focused libraries), can be planned effectively with retrosynthetic analysis.
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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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