Novel Flow Chemistry Application for Continuous Macrocyclisation

    Macrocyclic structures are common synthetic targets in drug discovery, interest is increasing in this field.    Macrocycles are common and broadly distributed in nature, and ∼20% of all known natural products from terrestrial and marine sources possess cyclic structures.   More than 100 macrocyclic compounds derived from natural products are used as commercial drugs, there is a continuing interest in exploring macrocyclic structures and macrocyclization reactions for the invention of new drugs.

    Macrocyclic compounds can be obtained using a variety of continuous flow reactions for the key ring-closing step.  This is an exciting area that flow chemistry is establishing its relevance towards

    Examples of published literature for Novel Flow Chemistry Application for Continuous Macrocyclisation

    High-Yielding Flow Synthesis of a Macrocyclic Molecular Hinge

    Christopher D. Jonesa, Laurence J. Kershaw Cooka, David Marquez-Gameza, Konstantin V. Luzyanina, Jonathan W. Steedb, Anna G. Slatera

    • aDepartment of Chemistry and Materials Innovation Factory, University of Liverpool, Crown Street, Liverpool L69 7ZD, U.K.
    • bDepartment of Chemistry, Durham University, South Road, Durham DH1 3LE, U.K.
    View abstract

    Synthesis of a Renewable Macrocyclic Musk: Evaluation of Batch, Microwave, and Continuous Flow Strategies

    Émilie Morin §, Johann Sosoe §, Michaël Raymond §, Benjamin Amorelli †*, Richard M. Boden †, Shawn K. Collins *§

    • § Department of Chemistry and Centre for Green Chemistry and Catalysis, Université de Montréal, CP 6128 Station Downtown, Montréal, Québec, Canada H3C 3J7
    • † Research & Development, International Flavors & Fragrances Inc., 1515 State Route 36, Union Beach, New Jersey, 07735, United States
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    Total Synthesis of Neomarchantin A: Key Bond Constructions Performed Using Continuous Flow Methods

    Émilie Morin, Michaël Raymond, Amaury Dubart, and Shawn K. Collins

    • Department of Chemistry and Centre for Green Chemistry and Catalysis, Université de Montréal, CP 6128 Station Downtown, Montréal, Québec, Canada H3C 3J7
    View abstract

    Phase separation macrocyclization in a complex pharmaceutical setting: application toward the synthesis of vaniprevir

    Eric Godin, Anne-Catherine Bédard, Michael Raymond, Shawn K. Collins*

    • Département de Chimie, Centre for Green Chemistry and Catalysis, Université de Montréal, CP 6128 Station Downtown, Montréal, Québec, H3C 3J7 Canada
    View abstract

    Catalytic macrocyclization strategies using continuous flow: formal total synthesis of ivorenolide A

    Mylène de Léséleuc, Eric Godin, Shawn Parisien-Collette, Alexandre Levesque, and Shawn K. Collins

    • University of Montréal, Department of Chemistry, Montréal, Canada
    View abstract

    Efficient Continuous-Flow Synthesis of Macrocyclic Triazoles

    Anne-Catherine Bédard, Jeffrey Santandrea, Shawn K. Collins

    • Department of Chemistry and Centre for Green Chemistry and Catalysis, University of Montreal
    View abstract

    Investigating the continuous synthesis of a nicotinonitrile precursor to nevirapine

    Ashley R. Longstreet1, Suzanne M. Opalka1, Brian S. Campbell1, B. Frank Gupton2, Tyler McQuade1

    • 1 Department of Chemistry and Biochemistry, Florida State University, United States
    • 1 Department of Chemistry, Virginia Commonwealth University, United States
    View abstract

    Regioselective Synthesis of 3-Aminoimidazo[1,2-a]-pyrimidines under Continuous Flow Conditions

    Ashlie J. E. Butler, Mark J. Thompson, Patrick J. Maydom, James A. Newby, Kai Guo, Harry Adams, Beining Chen*

    • Department of Chemistry, University of Sheffield, Sheffield, U.K.
    View abstract

    Continuous Synthesis of Artemisinin-Derived Medicines

    Kerry Gilmorea, Daniel Kopetzkia, Ju Weon Leeb, Zoltan Horvathb, D. Tyler McQuadea, Andreas Seidel-Morgensternb,c, Peter H. Seebergera,d

    • aMax-Planck-Institute of Colloids and Interfaces, Department of Biomolecular Systems, Germany
    • bMax-Planck-Institute for Dynamics of Complex Technical Systems, Germany
    • cOtto-von-Guericke-University, Chair for Chemical Process Technology, Germany
    • dFreie Universität Berlin, Institute of Chemistry and Biochemistry, Berlin, Germany
    View abstract

    Continuous Flow Synthesis of Thieno[2,3-c]isoquinolin-5(4H)-one Scaffold: A Valuable Source of PARP-1 Inhibitors

    Paolo Filipponi†, Carmine Ostacolo‡, Ettore Novellino‡, Roberto Pellicciari†§, Antimo Gioiello*†

    • †Dipartimento di Scienze Farmaceutiche, Università di Perugia, Via del Liceo 1, I-06123 Perugia, Italy
    • ‡Dipartimento di Farmacia, Università degli Studi di Napoli Federico II, Napoli, Italy §TES Pharma S.r.l., Corciano (Perugia), Italy
    View abstract

    Continuous flow macrocyclization at high concentrations: synthesis of macrocyclic lipids

    Anne-Catherine Bédard, Sophie Régnie, Shawn K. Collins

    • Département de Chimie, Centre for Green Chemistry, Catalysis, Université de Montréal, Montréal, Canada
    View abstract

    Scale-Up of Flow-Assisted Synthesis of C2-Symmetric Chiral PyBox Ligands

    Claudio Battilocchio1,3, Marcus Baumann1, Ian R. Baxendale1, Mariangela Biava3, Matthew O. Kitching1, Steven V. Ley1, Rainer E. Martin*2, Stephan A. Ohnmacht2, Nicholas D. C. Tappin1

    • 1Department of Chemistry, University of Cambridge, UK
    • 2F. Hoffmann-La Roche Ltd., Pharmaceuticals Division, Basel, Switzerland
    • 3Department of Pharmaceutical Chemistry and Technology, Sapienza University of Rome, Italy
    View abstract

    Synthesis of β-Keto Esters In-Flow and Rapid Access to Substituted Pyrimidines

    Hannah E. Bartrum1, David C. Blakemore2, Christopher J. Moody1, Christopher J. Hayes1

    • 1School of Chemistry, University of Nottingham, UK
    • 2Pfizer Global Research and Development, Sandwich, UK
    View abstract

    Application Notes regarding Novel Flow Chemistry Application for Continuous Macrocyclisation

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