Publications
Below are a selection of recent publications that showcase the Vapourtec technology.
Click here for list of peer reviewed publications
(or here to download whole list as a single PDF
)
Click here to see magazine articles.
Click here to see posters.
Click here to be kept up to date by email when more publications are added.
Continuous-Flow Synthesis of the Anti-Malaria Drug Artemisinin
François Lévesque1, Peter H. Seeberger1,2
http://dx.doi.org/10.1002/anie.201107446
Continuous proline catalysis via leaching of solid proline
Suzanne M. Opalka1, Ashley R. Longstreet2 and D. Tyler McQuade2
1Department of Chemistry and Chemical Biology, Cornell University, USA
2Department of Chemistry and Biochemistry, Florida State University,USA
http://dx.doi.org/10.3762/bjoc.7.197
Application of Flow Chemistry to the Selective Reduction of Esters to Aldehydes
Juan de M. Muñoz1, Jesús Alcázar1, Antonio de la Hoz2, Angel Díaz-Ortiz2
1Janssen, Toledo, Spain
2Facultad de Ciencias Químicas, Universidad de Castilla-La Mancha, Spain
http://dx.doi.org/10.1002/ejoc.201101458
Synthesis of Annulated Pyridines by Intramolecular Inverse-Electron-Demand Hetero-Diels-Alder Reaction under Superheated Continuous Flow Conditions
Rainer E. Martin1, Falk Morawitz1, Christoph Kuratli1, André M. Alker2, Alexander I. Alanine1
1Chemistry Technology and Innovation, F. Hoffmann-La Roche Ltd, Basel, Switzerland
2Biostructure Section, F. Hoffmann-La Roche Ltd,Basel, Switzerland
http://dx.doi.org/10.1002/ejoc.201101538
The application of a monolithic triphenylphosphine reagent for conducting Appel reactions in flow microreactors
Kimberley A. Roper1, Heiko Lange1, Anastasios Polyzos1, Malcolm B. Berry2,
Ian R. Baxendale1 and Steven V. Ley1
1Innovative Technology Centre, University of Cambridge
2GlaxoSmithKline, Stevenage, UK
http://dx.doi.org/10.3762/bjoc.7.194
Continuous Preparation of Arylmagnesium Reagents in Flow with Inline IR Monitoring
Tobias Brodmann¹, Peter Koos¹, Albrecht Metzger¹, Paul Knochel*², Steven V. Ley*¹
¹Department of Chemistry, University of Cambridge, U.K.
²Department of Chemistry, Ludwig Maximilians-Universität München, Germany
http://dx.doi.org/10.1021/op200275d
New Insights into Cyclobutenone Rearrangements: A Total Synthesis of the Natural ROS-Generating Anti-Cancer Agent Cribrostatin (ROS=reactive-oxygen species)
Mubina Mohamed¹, Théo P. Gonçalves¹, Richard J. Whitby¹, Helen F. Sneddon², David C. Harrowven¹
¹Dept of Chemistry, University of Southampton, UK
²GSK Medicines Research Centre, Stevenage, UK
http://dx.doi.org/10.1002/chem.201102263
The Oxygen-Mediated Synthesis of 1,3-Butadiynes in Continuous Flow: Using Teflon AF-2400 to Effect Gas/Liquid Contact
Trine P. Petersen 123, Anastasios Polyzos 14, Matthew O’Brien 1, Trond Ulven 2,
Ian R. Baxendale 1 , Steven V. Ley 1
1 Whiffen Laboratory, University of Cambridge, UK
2 Department of Physics and Chemistry, University of Southern Denmark
3 Discovery Chemistry and DMPK, H. Lundbeck A/S,Denmark
4 CSIRO, Materials Science and Engineering, Australia
http://dx.doi.org/10.1002/cssc.201100339
Lead Diversification 2: Application to P38, gMTP and lead compounds
M. Abid Masood ¹, Marc Bazin², Mark E. Bunnage¹, Andrew Calabrese³, Mark Cox¹, Sally-Ann Fancy¹,
Elizabeth Farrant¹, David W. Pearce¹, Manuel Perez¹, Laure Hitzel¹, Torren Peakman¹
¹ Worldwide Medicinal Chemistry, Pfizer, UK
² Hepatochem, Cambridge, MA, USA
³ Celgene San Diego, USA
http://dx.doi.org/10.1016/j.bmcl.2011.11.033
A continuous-flow synthesis of annulated and polysubstituted furans from the reaction of ketones and a-haloketones
Mark York
CSIRO Materials Science and Engineering, Australia
Cooperative Research Centre for Polymers, Notting Hill, Australia
http://dx.doi.org/10.1016/j.tetlet.2011.09.083
Suzuki-Miyaura Cross-Coupling of Heteroaryl Halides and Arylboronic Acids in Continuous Flow
Timothy Noël and Andrew J. Musacchio
Department of Chemistry, MIT, USA
http://dx.doi.org/10.1021/ol202052q
The Oxygen-Mediated Synthesis of 1,3-Butadiynes in Continuous Flow: Using Teflon AF-2400 to Effect Gas/Liquid Contact
Continuous flow synthesis of conjugated polymers
Helga Seyler, David J. Jones, Andrew B. Holmes and Wallace W. H. Wong
Bio21 Institute, University of Melbourne, Australia
http://dx.doi.org/10.1039/C1CC14315H
Continuous-flow, palladium-catalysed alkoxycarbonylation reactions using a prototype reactor in which it is possible to load gas and heat simultaneously
Michael A. Mercadante and Nicholas E. Leadbeater
Department of Chemistry, University of Connecticut, USA
http://dx.doi.org/10.1039/C1OB05808H
Teflon AF-2400 mediated gas–liquid contact in continuous flow methoxycarbonylations and in-line FTIR measurement of CO concentration
Peter Koos, Ulrike Gross, Anastasios Polyzos, Matthew O'Brien, Ian Baxendale and Steven V. Ley
Innovative Technology Centre, University of Cambridge, UK
http://dx.doi.org/10.1039/C1OB06017A
Rapid Access to -Alkoxy and -Amino Acid Derivatives through Safe Continuous-Flow Generation of Diazoesters
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
http://dx.doi.org/10.1002/chem.201101590
Continuous flow photolysis of aryl azides: Preparation of 3H-azepinones
Farhan R. Bou-Hamdan,François Lévesque, Alexander G. O'Brien, Peter H. Seeberger
Max Planck Institute of Colloids and Interfaces, Berlin, Germany
http://dx.doi.org/10.3762/bjoc.7.129
Ozonolysis in Flow Using Capillary Reactors
M. D. Roydhouse1, A. Ghaini2, A. Constantinou, A. Cantu-Perez2, W. B. Motherwell1, and A. Gavriilidis2
1Department of Chemistry, University College London, UK
2Department of Chemical Engineering, University College London, UK
http://dx.doi.org/10.1021/op200036d
Nitrile Oxide 1,3-Dipolar Cycloaddition by Dehydration of Nitromethane Derivatives Under Continuous Flow Conditions
Malte Brasholz, Simon Saubern* and G. Paul Savage
CSIRO Materials Science and Engineering, Victoria, Australia.
http://dx.doi.org/10.1071/CH11079
Nitration Chemistry in Continuous Flow using Fuming Nitric Acid in a Commercially Available Flow Reactor
Cara E. Brocklehurst, Hansjrg Lehmann, and Luigi La Vecchia
Global Discovery Chemistry, Novartis, Basel, Switzerland
http://dx.doi.org/10.1021/op200055r
Synthesis of (+)-Dumetorine and Congeners by Using Flow Chemistry Technologies
Elena Riva2, Anna Rencurosi1, Stefania Gagliardi1, Daniele Passarella2, Marisa Martinelli1*
1NiKem Research S.r.l., Milan, Italy
2Università degli Studi di Milano,Milan, Italy
http://dx.doi.org/10.1002/chem.201100300
Preparation of fluoxetine by multiple flow processing steps
Batoul Ahmed-Omer, Adam J. Sanderson
Eli Lilly and Co. Ltd., Lilly Research Centre, UK.
http://dx.doi.org/10.1039/C0OB00906G
Oxidation Reactions in Segmented and Continuous Flow Chemical Processing Using an N-(tert-Butyl)phenylsulfinimidoyl Chloride Monolith
Heiko Lange, Matthew J. Capener, Alexander X. Jones, Catherine J. Smith, Nikzad Nikbin, Ian R. Baxendale, Steven V. Ley*
Innovative Technology Centre, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK
http://dx.doi.org/10.1055/s-0030-1259923
Decarboxylative biaryl synthesis in a continuous flow reactor
¹Paul P. Lange , ¹Lukas J. Gooßen , ²Philip Podmore , ²Toby Underwood, ²Nunzio Sciammetta
¹Technische Universität Kaiserslautern, Germany
²Pfizer Global R&D, Sandwich, UK
http://dx.doi.org/10.1039/C0CC05708H
Diastereoselective Chain-Elongation Reactions Using Microreactors for Applications in Complex Molecule Assembly
Catherine F. Carter¹, Heiko Lange¹, Daiki Sakai², Ian R. Baxendale¹, Steven V. Ley¹
¹ Innovative Technology Centre, University of Cambridge, UK, CB2 1EW, UK
² Mitsubishi Tanabe Pharma Corporation, Yokohama, Japan
http://dx.doi.org/10.1002/chem.201003148
One-Flow, Multistep Synthesis of Nucleosides by Brønsted Acid-Catalyzed Glycosylation
Adam Sniady, Matthew W. Bedore, Timothy F. Jamison
Novartis Institutes for Biomedical Research Inc., Cambridge, USA
MIT, Cambridge, USA
http://dx.doi.org/10.1002/ange.201006440
An Integrated Flow and Batch-Based Approach for the Synthesis of O-Methyl Siphonazole
Marcus Baumann, Ian R. Baxendale, Malte Brasholz, John J. Hayward, Steven V. Ley, Nikzad Nikbin
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1039/C0OB00813C
Flow synthesis of organic azides and the multistep synthesis of imines and amines using a new monolithic triphenylphosphine reagent
Catherine J. Smith, Christopher D. Smith, Nikzad Nikbin, Steven V. Ley , Ian R. Baxendale
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1039/C0OB00813C
A fully automated, multistep flow synthesis of 5-amino-4-cyano-1,2,3-triazoles
Catherine J. Smith, Nikzad Nikbin, Steven V. Ley, Heiko Lange , Ian R. Baxendale
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1039/C0OB00815J
A General, One-Step Synthesis of Substituted Indazoles using a Flow Reactor
Rob C. Wheeler, Emma Baxter, Ian B. Campbell, Simon J. F. Macdonald
GlaxoSmithKline, Stevenage, UK
http://pubs.acs.org/doi/abs/10.1021/op100288t
Continuous flow synthesis of fullerene derivatives
Helga Seyler, Wallace Wing Ho Wong, Dave Jones , Andrew B. Holmes
University Of Melbourne, Australia
http://dx.doi.org/10.1021/jo2001879
Controlled RAFT Polymerization in a Continuous Flow Microreactor
Christian H. Hornung ,Carlos Guerrero-Sanchez, Malte Brasholz, Simon Saubern, John Chiefari, Graeme Moad, Ezio Rizzardo, San H. Thang
CSIRO Materials Science & Engineering, Victoria, Australia
http://dx.doi.org/10.1021/op1003314
Highly efficient dehydration of carbohydrates to 5-(chloromethyl)furfural (CMF), 5-(hydroxymethyl)furfural (HMF) and levulinic acid by biphasic continuous flow processing
Malte Brasholz , Karin von Känel, Christian H. Hornung, Simon Saubern, John Tsanaktsidis
CSIRO Materials Science & Engineering, Victoria , Australia
http://dx.doi.org/10.1039/C1GC15107J
A fully automated, multistep flow synthesis of 5-amino-4-cyano-1,2,3-triazoles
Catherine J. Smith, Nikzad Nikbin, Steven V. Ley, Heiko Lange and Ian R. Baxendale
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1039/C0OB00815J
Continuous flow thermolysis of azidoacrylates for the synthesis of heterocycles and pharmaceutical intermediates
Alexander G. O'Brien, François Lévesque and Peter H. Seeberger
Max Planck Institute of Colloids and Interfaces, Potsdam, Germany
http://dx.doi.org/10.1039/C0CC04481D
Safe and Reliable Synthesis of Diazoketones and Quinoxalines in a Continuous Flow Reactor
Laetitia J. Martin1, Andreas L. Marzinzik1, Steven V. Ley2, Ian R. Baxendale2
1 Novartis Institute for BioMedical Research, Basel, Switzerland
2 Innovative Technology Centre, Department of Chemistry, University of Cambridge
http://dx.doi.org/10.1021/ol1027927
The Continuous-Flow Synthesis of Carboxylic Acids using CO2 in a Tube-In-Tube Gas Permeable Membrane Reactor
Anastasios Polyzos, Matthew O’Brien, Trine P. Petersen, Ian R. Baxendale, Steven V. Ley
Innovative Technology Centre, Department of Chemistry, University of Cambridge
http://dx.doi.org/10.1002/anie.201006618
Continuous Flow Coupling and Decarboxylation Reactions Promoted by Copper Tubing
Yun Zhang1, Timothy F. Jamison2, Sejal Patel1, Nello Mainolfi1
1 Novartis Institutes for Biomedical Research Inc., Cambridge, USA
2 MIT, Cambridge, USA
http://dx.doi.org/10.1021/ol1026848
Synthesis of β-Keto Esters In-Flow and Rapid Access to Substituted Pyrimidines
Hannah E. Bartrum1, David C. Blakemore2, Christopher J. Moody1, and Christopher J. Hayes1
1 School of Chemistry, University of Nottingham, UK
2 Pfizer Global Research and Development, Sandwich, UK
http://dx.doi.org/10.1021/jo101783m
Synthesis of 3-Aryl/benzyl-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole Derivatives: A Comparison between Conventional, Microwave-Assisted and Flow-Based Methodologies
Sabrina Castellano1, Lucia Tamborini2, Monica Viviano1, Andrea Pinto2, Gianluca Sbardella1, and Paola Conti2
1 Dipartimento di Scienze Farmaceutiche, Universit degli Studi di Salerno, Via Ponte Don Melillo, 84084 Fisciano, Italy
2 Dipartimento di Scienze Farmaceutiche “Pietro Pratesi”, Universit degli Studi di Milano , Italy
http://dx.doi.org/10.1021/jo1014323
Flow synthesis of tricyclic spiropiperidines as building blocks for the histrionicotoxin family of alkaloids
Malte Brasholz1 , Brian A. Johnson2, James M. Macdonald1 , Anastasios Polyzos1 , John Tsanaktsidis1 , Simon Saubern1 , Andrew B. Holmes1,2 and John H. Ryan1 ,
1 CSIRO Molecular and Health Technologies, Victoria, Australia
2 School of Chemistry, Bio 21 Institute, University of Melbourne, Victoria, Australia http://dx.doi.org/10.1016/j.tet.2010.04.092
A Gram-Scale Batch and Flow Total Synthesis of Perhydrohistrionicotoxin
Dr. Malte Brasholz1, Dr. James M. Macdonald1, Dr. Simon Saubern1, Dr. John H. Ryan1, Prof. Dr. Andrew B. Holmes1, 2
1 CSIRO Molecular and Health Technologies, Victoria, Australia
2 School of Chemistry, Bio 21 Institute, University of Melbourne, Victoria, Australia
http://dx.doi.org/10.1002/chem.201090183
Effect of phase transfer chemistry, segmented fluid flow, and sonication on the synthesis of cinnamic esters
Mauro Riccaboni, Elena La Porta, Andrea Martorana and Roberta Attanasio
Department of Medicinal Chemistry, NiKem Research Srl, Milan, Italy
http://dx.doi.org/10.1016/j.tet.2010.04.031
Continuous Flow Palladium(II)-Catalyzed Oxidative Heck Reactions with Arylboronic Acids
Luke R. Odell 1, Jonas Lindh 1, Tomas Gustafsson 2, Mats Larhed 1 *
1 Organic Pharmaceutical Chemistry, Department of MedChem, Uppsala University, Sweden
2 AstraZeneca R&D Mölndal, Sweden
http://dx.doi.org/10.1002/ejoc.201000063
Reaction of Grignard reagents with carbonyl compounds under continuous flow conditions
E. Riva1, S. Gagliardi2, M. Martinelli2, D. Passarella1, D. Vigo2 and A. Rencurosi2,
1 Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy
2 NiKem Research S.r.l., , Milan, Italy
http://dx.doi.org/10.1016/j.tet.2010.02.078
[3+2] Dipolar cycloadditions of an unstabilised azomethine ylide under continuous flow conditions
Mark Grafton, Andrew C. Mansfield and M. Jonathan
Pfizer Global Research and Development, Sandwich, UK
http://dx.doi.org/10.1016/j.tetlet.2009.12.071
A highly efficient flow reactor process for the synthesis of N-Boc-3,4-dehydro-l-proline methyl ester
Lucia Tamborini, Paola Conti, Andrea Pinto and Carlo De Micheli
Dipartimento di Scienze Farmaceutiche ‘Pietro Pratesi’,
Università degli Studi di Milano, Italy
http://dx.doi.org/10.1016/j.tetasy.2009.12.023
Efficient Continuous Flow Synthesis of Hydroxamic Acids and Suberoylanilide Hydroxamic Acid Preparation
E. Riva1, S. Gagliardi2, Caterina Mazzoni 2, M. Martinelli2, D. Passarella1, D. Vigo2 and A. Rencurosi2,
1 Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Italy
2 NiKem Research S.r.l., Milan, Italy
http://dx.doi.org/10.1021/jo900144h
The application of flow microreactors to the preparation of a family of casein kinase I inhibitors
Francesco Venturoni, Nikzad Nikbin, Steven V. Ley and Ian R. Baxendale
Innovative Technology Centre, Department of Chemistry, University of Cambridge
http://dx.doi.org/10.1039/b925327k
Multi-Step Synthesis by Using Modular Flow Reactors: The Preparation of YneOnes and Their Use in Heterocycle Synthesis
Ian R. Baxendale1, Søren C. Schou2, Jörg Sedelmeier1, Steven V. Ley1
1ITC, Department of Chemistry, University of Cambridge
2LEO Pharma, Medicinal Chemistry Research, Denmark
http://dx.doi.org/10.1055/s-0029-1219431
A Flow Process Using Microreactors for the Preparation of a Quinolone Derivative as a Potent 5HT1B Antagonist
Zizheng Qian, Ian R. Baxendale, Steven V. Ley
Innovative Technology Centre, Department of Chemistry, University of Cambridge
http://dx.doi.org/10.1055/s-0029-1219358
A flow-based synthesis of Imatinib: the API of Gleevec
Mark D. Hopkin, Ian R. Baxendale and Steven V. Ley
Innovative Technology Centre, Department of Chemistry, University of Cambridge
http://dx.doi.org/10.1039/c001550d
ReactIR Flow Cell: A New Analytical Tool for Continuous Flow Chemical Processing
Catherine F. Carter1, Heiko Lange1, Steven V. Ley1, Ian R. Baxendale1, Brian Wittkamp2, Jon G. Goode3 and Nigel L. Gaunt3
1 Innovative Technology Centre, Department of Chemistry, University of Cambridge
2 Mettler-Toledo AutoChem, USA
3 Mettler-Toledo AutoChem, UK
http://dx.doi.org/10.1021/op900305v
A safe and reliable procedure for the iododeamination of aromatic and heteroaromatic amines in a continuous flow reactor
Laia Malet-Sanz , Julia Madrzak, Rhian S. Holvey and Toby Underwood
Research Chemistry, Pfizer Global Research and Development, Sandwich, UK
http://dx.doi.org/10.1016/j.tetlet.2009.10.007
Development of fluorination methods using continuous-flow microreactors
Marcus Baumann, Ian R. Baxendale, Laetitia J. Martin, Steven V. Ley
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1016/j.tet.2009.05.083
Multistep Synthesis Using Modular Flow Reactors: Bestmann-Ohira Reagent for the Formation of Alkynes and Triazoles
Ian R. Baxendale1, Steven V. Ley1, Andrew C. Mansfield 2, Christopher D. Smith1
1ITC, Department of Chemistry, University of Cambridge,
2Pfizer Global R&D Research Centre, Sandwich, (UK)
http://dx.doi.org/10.1002/anie.200900970
A Bifurcated Pathway to Thiazoles and Imidazoles Using a Modular Flow Microreactor
Ian R. Baxendale, Steven V. Ley, Christopher D. Smith, Lucia Tamborini and Ana-Florina Voica
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1021/cc800070a
The Use of Diethylaminosulfur Trifluoride (DAST) for Fluorination in a Continuous-Flow Microreactor
Baumann, Marcus, Baxendale, Ian R., Ley, Steven V.
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1055/s-2008-1078026
A modular flow reactor for performing Curtius rearrangements as a continuous flow process
Marcus Baumann1, Ian R. Baxendale1, Steven V. Ley1, Nikzad Nikbin1, Christopher D. Smith1 and Jason P. Tierney2
1 Innovative Technology Centre, Department of Chemistry, University of Cambridge
2 Neurology Lead Discovery Chemistry, GlaxoSmithKline R and D, Harlow, UK
http://dx.doi.org/10.1039/b801631n
Azide monoliths as convenient flow reactors for efficient Curtius rearrangement reactions
Marcus Baumann, Ian R. Baxendale, Steven V. Ley, Nikzad Nikbin and Christopher D. Smith
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1039/b801634h
A flow reactor process for the synthesis of peptides utilizing immobilized reagents, scavengers and catch and release protocols
Ian R. Baxendale, Steven V. Ley, Christopher D. Smith and Geoffrey K. Tranmer
Innovative Technology Centre, Cambridge, UK
http://dx.doi.org/10.1039/b612197g
Fully Automated Flow-Through Synthesis of Secondary Sulfonamides in a Binary Reactor System
Charlotte M. Griffiths-Jones, Mark D. Hopkin, Daniel Jönsson, Steven V. Ley, David J. Tapolczay, Emma Vickerstaffe, and Mark Ladlow
GlaxoSmithKline Cambridge Technology Centre, Cambridge
http://dx.doi.org/10.1021/cc060152b
Continuous Flow Ligand-Free Heck Reactions Using Monolithic Pd [0] Nanoparticles
Nikzad Nikbin, Mark Ladlow, and Steven V. Ley
Department of Chemistry, University of Cambridge, UK
http://dx.doi.org/10.1021/op7000436
Tagged phosphine reagents to assist reaction work-up by phase-switched scavenging using a modular flow reactor
Christopher D. Smith, Ian Baxendale, Geoffrey Tranmer, Marcus Baumann, Stephen Smith, Russell Lewthwaite and Steven V. Ley
Department of Chemistry, University of Cambridge, UK
http://dx.doi.org/10.1039/b703033a
| Articles: |
| Follow the Pharma Flow (published in Speciality Chemicals magazine) |