Diversity Oriented Synthesis

Diversity Oriented Synthesis

  • Madhukar Baburao Deshmukh added an answer:
    What is divergent synthesis & convergent synthesis?

    I have prepared same compounds in different (4) routes. Can I call this as a divergent (Diversity Oriented) synthesis or convergent synthesis?

    Madhukar Baburao Deshmukh

    Convergent synthesis involves the synthesis & isolation, Similarly  another is synthesised . Then these two  mixed together to get target compd.This is known as branched strategy of Convergent synthesis which gives better yields of the products tha linear approach.

  • Antonio Guarna added an answer:
    diversity oriented synthesis(DOS) is an emerging area in creating a small molecule libraries. Since it is since still in its infacy, there is a great opportunity to the synthetic chemists to discover novel lead molecules by putting efforts in this field in comig days. Till now there is no much rational efforts in this field.
    Antonio Guarna
    to have a complete picture of the potentiality of DOS , I may suggest you to read the book edited by Andrea Trabocchi, recently published by Wiley. https://www.researchgate.net/publication/249011185_Diversity-Oriented_Synthesis_Basics_and_Applications_in_Organic_Synthesis_Drug_Discovery_and_Chemical_Biology
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      ABSTRACT: http://onlinelibrary.wiley.com/book/10.1002/9781118618110 http://www.wiley.com/WileyCDA/WileyTitle/productCd-1118145658,subjectCd-CHD0.html Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. 1 The Basics of Diversity-Oriented Synthesis Kieron M. G. O’Connell, Warren R. J. D. Galloway, and David R. Spring PART I CHEMICAL METHODOLOGY IN DIVERSITY-ORIENTED SYNTHESIS 2 Strategic Applications of Multicomponent Reactions in Diversity-Oriented Synthesis John M. Knapp, Mark J. Kurth, Jared T. Shaw, and Ashkaan Younai 3 Cycloaddition Reactions in Diversity-Oriented Synthesis Giovanni Muncipinto 4 Phosphine Organocatalysis as a Platform for Diversity-Oriented Synthesis Zhiming Wang and Ohyun Kwon 5 Domino Reactions in Library Synthesis Matthew G. LaPorte, John R. Goodell, Sammi Tsegay, and Peter Wipf 6 Diversity-Oriented Synthesis of Amino Acid–Derived Scaffolds and Peptidomimetics: A Perspective Andrea Trabocchi 7 Solid-Phase Synthesis Enabling Chemical Diversity Nadezda Cankarova and Viktor Krchnak 8 Macrocycles as Templates for Diversity Generation in Drug Discovery Eric Marsault PART II CHEMICAL LIBRARIES AND DIVERSITY-ORIENTED SYNTHESIS 9 Diversity-Oriented Synthesis of Natural Product–Like Libraries Mark Dow, Francesco Marchetti, and Adam Nelson 10 Chemoinformatic Characterization of the Chemical Space and Molecular Diversity of Compound Libraries José Luis Medina-Franco 11 DNA-Encoded Chemical Libraries Luca Mannocci PARTIII SCREENING METHODS AND LEAD IDENTIFICATION 12 Experimental Approaches to Rapid Identification, Profiling, and Characterization of Specific Biological Effects of DOS Compounds Eduard A. Sergienko and Susanne Heynen-Genel 13 Small-Molecule Microarrays Hongyan Sun 14 Yeast as a Model in High-Throughput Screening of Small-Molecule Libraries Irene Stefanini, Carlotta De Filippo, and Duccio Cavalieri 15 Virtual Screening Methods Jurgen Bajorath 16 Structure–Activity Relationship Data Analysis: Activity Landscapes and Activity Cliffs Jurgen Bajorath PARTIV APPLICATIONS IN CHEMICAL BIOLOGY AND DRUG DISCOVERY 17 Diversity-Oriented Synthesis and Drug Development: Facilitating the Discovery of Novel Probes and Therapeutics Jeremy R. Duvall, Eamon Comer, and Sivaraman Dandapani 18 DOS-Derived Small-Molecule Probes in Chemical Biology Nicholas Hill, Lingyan Du, and Qiu Wang
      Edited by Andrea Trabocchi, 06/2013; John Wiley & Sons, Inc.., ISBN: 9781118145654
  • Pierre-André Fournier added an answer:
    Does the synthetic scheme attached herewith have any faults?
    We are working on the synthesis of a HIV NRTI. We want to protect the -OH end of the starting element with TMS-Cl. What would be the best reagent to deprotect TMS-Cl in case of this reaction? Will it be done by any acid, NaF or tetra-n-butylammonium fluoride? Which one will be better in this case? Please give your views on any other issues with thissynthetic scheme?
    Pierre-André Fournier
    Cyclopropyl bromide is a terrible electrophile. The cyclopropanes have a strong sp2 character (the bonds are actually "bend" to accommodate the 60° angle of triangles and the 109 angles of sp3 bonds). I would look at a Chan-Lam coupling with the cyclopropyl boronic acid (copper promoted cross coupling between amines, most commonly anilines, and boronic acids). Mono-coupling is not an issue in these cases.

    Chemical Communications (Cambridge, United Kingdom), 46(19), 3393-3395; 2010.

    Also, as Mr. Dera stated, alkylation of amines is a greatly over-rated reaction as the overalkylation problem is very common. Reductive amination or cross-coupling are far better alternatives. And as for a TMS-deprotection of a primary alcohol, some 1N HCl in THF should do the job instantly as TMS is very easy to remove (maybe too easy for a Chan-Lam coupling...). I don't think a primary alcohol is incompatible with most cross-coupling, so I'd first try a direct reaction.

About Diversity Oriented Synthesis

design and synthesis of skeletally diversified library of molecules from privilized structures

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