Biological

Mimicking natural metabolisms: cell‐free flow preparation of dopamine

Silvia Donzella^a, Agostina Colacicco^a, Luca Nespoli^a, Dr. Martina L. Contente^a

• ^aDepartment of Food, Environmental and Nutritional Sciences (DeFENS), University of Milan, via Celoria, 2, 20133 Milan, Italy

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Innovation in delivering synthetically challenging bicyclic arginase inhibitors to enhance immunotherapy

Derun Li^a, Hongjun Zhang^a, Thomas W. Lyons^a, Theodore A. Martinot^a, Abdelghani Achab^a, Min lu^a, Lisa M. Nogle^a, Spencer McMinn^a, Matthew J. Mitcheltree^a, Matthew Childers^a, Qinglin Pu^a, Symon Gathiaka^a, Anand Palani^a, Kalyan Chakravarthy^a, Amy D. DeCastro^a, Jennifer O'Neil^a, Roshi Afshar^a, Nicole C. Walsh^a, Peter W. Fan^a, Mangeng Cheng^a, Richard Miller^a, Amy Doty^a, Rachel Palte^a, Hai-Young Kim^a, Josep Saurí^a, Adam Beard^a, Christopher Brynczka^a and Christian Fischer^a

• ^aMerck Research Laboratory, Boston, MA.

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Cellulose fast pyrolysis for platform chemicals: assessment of potential targets and suitable reactor technology

Anurag Parihar, Sankar Bhattacharya

• Department of Chemical Engineering, Monash University, Clayton, VIC, Australia

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Flow nanoprecipitation of size-controlled D-leucine nanoparticles for spray-drying formulations

Bruno Cerra, Gabriele Mosca, Maurizio Ricci, Aurélie Schoubben and Antimo Gioiello

• Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, I-06122 Perugia, Italy

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Transaminase‐catalyzed continuous synthesis of biogenic aldehydes

Martina L. Contente ^a, Francesca Paradisi ^*a,b

• ^a School of Chemistry, University of Nottingham, University Park, Nottingham, NG7, 2RD, United Kingdom
• ^b Department of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, 3012 Bern

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Self-Sufficient Flow-Biocatalysis by Coimmobilization of Pyridoxal 5′-Phosphate and ω-Transaminases onto Porous Carriers

Ana I. Benítez-Mateos ^†, Martina L. Contente ^§, Susana Velasco-Lozano ^⊥, Francesca Paradisi ^*§, Fernando López-Gallego ^*⊥‡

• ^† Heterogeneous Biocatalysis Laboratory, CICbiomaGUNE, Paseo Miramón 182, Edificio empresarial C”, 20014 San Sebastián, Spain
• ^§ School of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, U.K
• ^⊥ Heterogeneous biocatalysis laboratory, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH−CSIC), University of Zaragoza, C/Pedro Cerbuna 12, 50009 Zaragoza, Spain
• ^‡ ARAID, Aragon I+D foundation, Zaragoza, Spain

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Self-sustaining closed-loop multienzyme-mediated conversion of amines into alcohols in continuous reactions

Martina L. Contente, Francesca Paradisi

• School of Chemistry, University of Nottingham, Nottingham, United Kingdom

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Dichlorophenylacrylonitriles as AhR Ligands displaying selective breast cancer cytotoxicity in vitro

Jennifer R Baker¹, Jayne Gilbert², Stefan Paula³, Xiao Zhu³, Jennette A Sakoff², Adam McCluskey¹

• ¹ The University of Newcastle, Chemistry, Newcastle, Australia
• ² Calvary Mater Hospital, Medical Oncology, Newcastle, Australia
• ³ Purdue University, Chemistry, West Lafayette, United States

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A combination of flow and batch mode processes for the efficient preparation of mGlu2/3 receptor negative allosteric modulators (NAMs)

Raveendra Panickar Dhanya, Ananda Herath, Douglas J. Sheffler, Nicholas D.P. Cosford

• Cancer Metabolism and Signaling Networks Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 N. Torrey Pines Rd., La Jolla, CA 92037, USA

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Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification

Serena Mostarda^a, Daniela Passeri^b, Andrea Carotti^a,1, Bruno Cerra^a, Carolina Colliva^b, Tiziana Benicchi^b, Antonio Macchiarulo^a, Roberto Pellicciari^b, Antimo Gioiello^a

• ^a Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo, 1, 06123 Perugia, Italy
• ^b TES Pharma, Corso Vannucci, 47, 06121 Perugia, Italy

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Targeting a mirabegron precursor by BH3-mediated continuous flow reduction process

Sonia De Angelis^a, Claudia Carlucci^a, Modesto de Candia^a, Gabriele Rebuzzini^b, Paolo Celestini^b, Massimiliano Riscazzi^b, Renzo Luisi^a, Leonardo Degennaro^a

• ^a FLAME-Lab − Flow Chemistry and Microreactor Technology Laboratory, Department of Pharmacy — Drug Sciences, University of Bari “A. Moro” Via E. Orabona 4, Bari 70125, Italy
• ^b COSMA S.p.A, Via Colleoni 15/17, Ciserano, BG 24040, Italy

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Highly efficient oxidation of amines to aldehydes with flow-based biocatalysis

Dr. Martina L. Contente^1,2, Federica Dall'Oglio³, Dr. Lucia Tamborini³, Prof. Francesco Molinari⁴, Prof. Francesca Paradisi^1,2

• ¹ School of Chemistry, University of Nottingham, Nottingham, UK
• ² UCD School of Chemistry, University College Dublin, Dublin, Ireland
• ³ Department of Pharmaceutical Sciences, DISFARM, University of Milan, Milan, Italy
• ⁴ Department of Food, Environmental and Nutritional Science, DeFENS, University of Milan, Milan, Italy

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Methanolysis of epoxidized soybean oil in continuous flow conditions

Vincenzo Pantone^a, Amelita Grazia Laurensa^b, Cosimo Annese^c, Francesco Fracassi^b, Caterina Fusco^b, Angelo Nacci^b,c, Antonella Russo^a, Lucia D’Accolti^b,c

• ^a Greenswitch s.r.l., Ferrandina MT, Italy
• ^b Dipartimento di Chimica, Università di Bari Aldo Moro, Via E. Orabona 4, 70126 Bari, Italy
• ^c ICCOM-CNR, SS Bari, Via E. Orabona 4, 70126 Bari, Italy

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Chemoenzymatic synthesis in flow reactors: a rapid and convenient preparation of captopril

Dr. Valerio De Vitis¹, Dr. Federica Dall'Oglio¹, Dr. Andrea Pinto², Prof. Carlo De Micheli², Prof. Francesco Molinari¹, Prof. Paola Conti², Dr. Diego Romano¹, Dr. Lucia Tamborini²

• ¹ Department of Food Environmental and Nutritional Science, University of Milan, Milan, Italy
• ² Department of Pharmaceutical Sciences, University of Milan, Milan, Italy

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Co-production of HMF and gluconic acid from sucrose by chemo-enzymatic method

Hongli Wu, Ting Huang, Fei Cao, Qiaogen Zou, Ping Wei, Pingkai Ouyang

• College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, 30 South Puzhu Road, Nanjing 211816 PR China

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Direct valorisation of waste cocoa butter triglycerides via catalytic epoxidation, ring-opening and polymerisation

Dorota D Plaza^a, Vinzent Strobel^b, Parminder Kaur KS Heer^b, Andrew B Sellars^d, Seng-Soi Hoong^d, Andrew J Clark^d, Alexei A Lapkin^b

• ^a School of Engineering, University of Warwick, Coventry, UK
• ^b Department of Chemical Engineering and Biotechnology, University of Cambridge, UK
• ^c Aachener Verfahrenstechnik – Process Systems Engineering, RWTH Aachen University, Aachen, Germany
• ^d Department of Chemistry, University of Warwick, Coventry, UK

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Utilizing on‐and off‐line monitoring tools to follow a kinetic resolution step during flow synthesis

Kathleen A. Farley, Usa Reilly, Dennis P. Anderson, Brian P. Boscoe, Mark W. Bundesmann, David A. Foley, Manjinder S. Lall, Chao Li, Matthew R. Reese, Jiangli Yan

• Medicinal Sciences, Pfizer Worldwide Research and Development, Groton, CT, United States

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Continuous-flow synthesis of highly functionalized imidazo-oxadiazoles facilitated by microfluidic extraction

Ananda Herath, Nicholas D. P. Cosford

• Cancer Metabolism & Signaling Networks Program, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, USA

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Active Site-Mapping of Xylan-Deconstructing Enzymes with Arabinoxylan Oligosaccharides Produced by Automated Glycan Assembly

Deborah Senf, Colin Ruprecht, Goswinus de Kruijff, Sebastian Simonetti, Frank Schuhmacher, Peter Seeberger, Fabian Pfrengle

• Max-Planck-Institute of Colloids and Interfaces, Biomolecular Systems, Potsdam, Germany

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Mixed-Linkage Glucan Oligosaccharides Produced by Automated Glycan Assembly Serve as Tools to Determine the Substrate Specificity of Lichenase

Pietro Dallabernardina, Frank Schuhmacher, Peter H Seeberger, Fabian Pfrengle

• Max-Planck-Institute of Colloids and Interfaces, Biomolecular Systems, Potsdam, Germany

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γ-Glutamyl-dipeptides: Easy tools to rapidly probe the stereoelectronic properties of the ionotropic glutamate receptor binding pocket

Lucia Tamborini^a, Veronica Nicosia^a, Paola Conti^a, Federica Dall'Oglio^a, Carlo De Micheli^a, Birgitte Nielsen^b, Anders A. Jensen^b, Darryl S. Pickering^b, Andrea Pinto^a

• ^a Department of Pharmaceutical Sciences (DISFARM), University of Milan, Via Mangiagalli 25, 20133 Milan, Italy
• ^b Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen OE, Denmark

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Continuous flow biocatalysis: production and in-line purification of amines by immobilised transaminase from Halomonas elongata

Matteo Planchestainer^a, Martina Letizia Contente^ab, Jennifer Cassidy^a, Francesco Molinari^b, Lucia Tamborini^*c, Francesca Paradisi^*ad

• ^* Corresponding authors
• ^a UCD School of Chemistry, University College Dublin, Belfield, Dublin 4, Ireland
• ^b Department of Food, Environmental and Nutritional Sciences (DeFENS), Università degli studi di Milano, Via Mangiagalli 25, Milan, Italy
• ^c Department of Pharmaceutical Sciences (DISFARM), Università degli studi di Milano, Via Mangiagalli 25, Milan, Italy
• ^d School of Chemistry, University of Nottingham, University Park, Nottingham, UK

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The generation of a library of bromodomain-containing protein modulators expedited by continuous flow synthesis

Paolo Filipponi and Ian R. Baxendale^*

• ^* Department of Chemistry, University of Durham South Road, Durham, DH1 3LE, United Kingdom

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Continuous flow photochemistry as an enabling synthetic technology: synthesis of substituted-6(5H)-phenanthridinones for use as poly(ADP-ribose) polymerase inhibitors

Y. Fang ^a, G. K. Tranmer ^*a,b

• ^* Corresponding authors ^a College of Pharmacy, Faculty of Health Sciences, University of Manitoba, Winnipeg, Canada
• ^b Department of Chemistry, Faculty of Science, University of Manitoba, Winnipeg, Canada

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Automated glycan assembly of xyloglucan oligosaccharides

Pietro Dallabernardina^{a b}, Frank Schuhmacher^{a b}, Peter H. Seeberger^{a b}, Fabian Pfrengle^{* a b}

• ^a Department of Biomolecular Systems, Max-Planck-Institute of Colloids and Interfaces, Am Mühlenberg 1, 14476 Potsdam, Germany
• ^b Freie Universität Berlin, Institute of Chemistry and Biochemistry, Arnimallee 22, 14195 Berlin, Germany

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An integrated flow and microwave approach to a broad spectrum protein kinase inhibitor

Cecilia Russell^a, Andrew J. S. Lin^a, Peter Hains^b, Michela I. Simone^a, Phillip J. Robinson^b, Adam McCluskey^{* a}

• ^A Centre for Chemical Biology, Chemistry, School of Environmental and Life Science, The University of Newcastle, University Drive, Callaghan, Australia
• ^B Children's Medical Research Institute, 214 Hawkesbury Road, Westmead, Australia

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A Short Multi-step Flow Synthesis of a Potential Spirocyclic Fragrance Component

Ian R. Baxendale*

• Department of Chemistry, University of Durham, South Road, Durham, DH1 3LE, UK

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Rapid Discovery of a Novel Series of Abl Kinase Inhibitors by Application of an Integrated Microfluidic Synthesis and Screening Platform

Bimbisar Desai, Karen Dixon, Elizabeth Farrant, Qixing Feng, Karl R. Gibson, Willem P. van Hoorn, James Mills, Trevor Morgan, David M. Parry, Manoj K. Ramjee, Christopher Nicholas Selway, Gary J. Tarver, Gavin Whitlock, Adrian G. Wright

• Cyclofluidic Ltd.

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Efficient synthesis of panaxadiol derivatives using continuous-flow microreactor and evaluation of anti-tumor activity

Yan Wu^a,1, Wei-Qi Chen^b,1, Yu-Qing Zhao^c, Hu-Ri Piao^a

• ^aKey Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, China
• ^bDepartment of Chemistry, Fudan University, Shanghai, China
• ^cSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, China

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An efficient continuous flow process for the synthesis of a non-conventional mixture of fructooligosaccharides

Paolo Zambelli^a, Lucia Tamborini^b, Samuele Cazzamalli^b, Andrea Pinto^b, Stefania Arioli^a, Silvia Balzaretti^a, Francisco J. Plou^c, Lucia Fernandez-Arrojo^c, Francesco Molinari^a, Paola Conti^b, Diego Romano^a

• ^a Department of Food Environmental and Nutritional Science (DeFENS), University of Milan, Via Mangiagalli, 20133 Milan, Italy
• ^b Department of Pharmaceutical Sciences (DISFARM), University of Milan, Via Mangiagalli 25, 20133 Milan, Italy
• ^c Instituto de Catálisis y Petroleoquímica, CSIC, 28049 Madrid, Spain

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Glucuronidation of bile acids under flow conditions: design of experiments and Koenigs–Knorr reaction optimization

Serena Mostarda^a, Paolo Filipponi^a, Roccaldo Sardella^a, Francesco Venturoni^a, Benedetto Natalini^a, Roberto Pellicciaria^b, Antimo Gioiello^*a

• ^aLaboratory of Medicinal and Advanced Synthetic Chemistry (Lab MASC), Department of Pharmaceutical Sciences, University of Perugia, Perugia, Italy
• ^bTES Pharma S.r.l., Corciano, Italy

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Seamless Integration of Dose-Response Screening and Flow Chemistry: Efficient Generation of Structure–Activity Relationship Data of ?-Secretase (BACE1) Inhibitors

Dr. Michael Werner^1,*, Christoph Kuratli¹, Dr. Rainer E. Martin^1,*, Dr. Remo Hochstrasser¹, David Wechsler¹, Dr. Thilo Enderle¹, Dr. Alexander I. Alanine¹, Prof. Dr. Horst Vogel²

• ¹ Medicinal Chemistry, Small Molecule Research, Pharma Research & Early Development (pRED), F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (Switzerland)
• ² Institute of Chemical Sciences and Engineering, Swiss Federal Institute of Technology of Lausanne (EPFL), Station 6, 1015 Lausanne (Switzerland)

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Biotransformation with whole microbial systems in a continuous flow reactor: resolution of (RS)-flurbiprofen using Aspergillus oryzae by direct esterification with ethanol in organic solvent

Lucia Tamborini^a, Diego Romano^b, Andrea Pinto^a, Martina Contente^a, Maria C. Iannuzzi^a, Paola Conti^a, Francesco Molinari^b

• ^a Dipartimento di Scienze Farmaceutiche, Universitá degli Studi di Milano, Italy
• ^b Dipartimento di Scienze per gli Alimenti, la Nutrizione e l'Ambiente (DEFENS), Universitá degli Studi di Milano, Italy

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Integrated Synthesis and Testing of Substituted Xanthine Based DPP4 Inhibitors: Application to Drug Discovery

Werngard Czechtizky, Jurgen Dedio, Bimbisar Desai, Karen Dixon, Elizabeth Farrant, Qixing Feng Trevor Morgen, David M Parry, Manoj K. Ramjee, Christopher N. Selway, Thorsten Schmidt, Gary J. Tarver, Adrian G. Wright

• Sanofi-Aventis, Frankfurt, Germany. Cyclofluidic Ltd., U.K.

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Synthesis of an H3 Antagonist via Sequential One-Pot Additions of a Magnesium Ate Complex and an Amine to a 1,4-Ketoester followed by Carbonyl-Directed Fluoride Addition

Joel M. Hawkins, Pascal Dubé, Mark T. Maloney, Lulin Wei. Marcus Ewing, Stephen M. Chesnut, Joshua R. Denette, Brett M. Lillie, Rajappa Vaidyanathan

• Pharmaceutical Sciences, Pfizer Inc., Groton, USA

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An efficient method for the lipase-catalysed resolution and in-line purification of racemic flurbiprofen in a continuous-flow reactor

Lucia Tamborini¹, Diego Romano², Andrea Pinto¹, Arianna Bertolani^1,2, Francesco Molinari², Paola Conti¹

• ¹Dipartimento di Scienze Farmaceutiche ‘Pietro Pratesi’, Universitá degli Studi di Milano, Italy
• ²Dipartimento di Scienze e Tecnologie Alimentari e Microbiologiche, Universitá degli Studi di Milano, Italy

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Lead Diversification 2: Application to P38, gMTP and lead compounds

M. Abid Masood¹, Marc Bazin², Mark E. Bunnage¹, Andrew Calabrese³, Mark Cox¹, Sally-Ann Fancy¹, Elizabeth Farrant¹, David W. Pearce¹, Manuel Perez¹, Laure Hitzel¹, Torren Peakman¹

• ¹Worldwide Medicinal Chemistry, Pfizer, UK
• ²Hepatochem, Cambridge, MA, USA
• ³Celgene San Diego, USA

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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

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