Esther Alza - Flow and Microreactor Technology in Medicinal Chemistry

1. Chapter 1
2. Chapter 2
3. Chapter 5
4. Chapter 7
5. Chapter 9

1. Chapter 1
2. Chapter 2
3. Chapter 3
4. Chapter 4
5. Chapter 5
6. Chapter 6
7. Chapter 7
8. Chapter 8
9. Chapter 9

Edited by

R. Mannhold, H. Buschmann, J. Holenz

Editorial Board

G. Folkers, H. Kubinyi, H. Timmermann, H. van deWaterbeemd, J. Bondo Hansen

Previous Volumes of the Series

Bachhav, Y. (Ed.)

Innovative Dosage Forms

Design and Development at Early Stage

2022

ISBN: 9783527343966

Vol. 81

RbsamenSchaeff, H., and Buschmann, H. (Eds.)

New Drug Development for Known and Emerging Viruses

2022

ISBN: 9783527343379

Vol. 80

Gruss, M. (Ed.)

Solid State Development and Processing of Pharmaceutical Molecules

Salts, Cocrystals, and Polymorphism

2021

ISBN: 9783527346356

Vol. 79

Plowright, A.T. (Ed.)

Target Discovery and Validation Methods and Strategies for Drug Discovery

2020

ISBN: 9783527345298

Vol. 78

Swinney, D., Pollastri, M. (Eds.)

Neglected Tropical Diseases Drug Discovery and Development

2019

ISBN: 9783527343041

Vol. 77

Bachhav, Y. (Ed.)

Innovative Dosage Forms Design and Development at Early Stage

2019

ISBN: 9783527343966

Vol. 76

Gervasio, F. L., Spiwok, V. (Eds.)

Biomolecular Simulations in Structurebased Drug Discovery

2018

ISBN: 9783527342655

Vol. 75

Sippl, W., Jung, M. (Eds.)

Epigenetic Drug Discovery

2018

ISBN: 9783527343140

Vol. 74

Giordanetto, F. (Ed.)

Early Drug Development

2018

ISBN: 9783527341498

Vol. 73

Handler, N., Buschmann, H. (Eds.)

Drug Selectivity

2017

ISBN: 9783527335381

Vol. 72

Edited by

Esther Alza

Volume Editor

Dr. Esther Alza
Alza & Associates S.L. Sustainable Chemistry Consulting
Rnda del Canig, Agr 7, 10
08950 Esplugues de Llobregat
Spain

Series Editors

Prof. Dr. Raimund Mannhold
Rosenweg 7
40489 Dsseldorf
Germany

Dr. Helmut Buschmann
Sperberweg 15
52076 Aachen
Germany

Dr. Jrg Holenz
BIAL PORTELA & CA., S.A.
So Mamede Coronado
Portugal

Cover
Background illustration: Pexels/Merlin

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Print ISBN: 9783527346899
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Recently, application of the flow technologies for the preparation of fine chemicals, such as natural products or active pharmaceutical ingredient s ( API s), has become very popular, especially in academia. Although pharma industry still relies on multipurpose batch or semibatch reactors, it is evident that interest is arising toward continuousflow manufacturing of organic molecules, including highly functionalized and chiral compounds. Therefore, it could be safely assumed that computercontrolled chemical synthesis using flow chemistry is becoming the key enabling technology for the chemistry laboratory of the future. Up to now these technologies were mainly being utilized in pharmaceutical industry in the field of the chemistry, manufacture, and control ( CMC ) by taking advantage of easy scaleup reactions. However, in the recent years many interesting articles by medicinal chemists have been reported, for example, the application of library synthesis in the hit and lead optimization field.

The book titled Flow and Microreactor Technology in Medicinal Chemistry An Emerging Technology Concept from Drug discovery to Process Development describes current and future uses in medicinal chemistry of this groundbreaking technology. Beside general chapters describing concepts of lab automation, several case studies explain the broad field of current and future applications of flow technology in the different phases of drug discovery and development from early hit and lead optimization to process development of multistep reactions. The contributing authors, all very well known as experts in this field, create a deep overview of the current status in the field and provide a solid ground that the reader will be inspired for future application. The following chapters give insight into this emerging technology:

• Chemistry at the Extremes: Turning Complex Reactions into Scalable Processes
• Automated Flow Chemistry Platforms
• Flow Chemistry Opportunities for Drug Discovery
• Flow Chemistry in Medicinal Chemistry Applications to BcrAbl Kinase Inhibitors
• Integrated Systems for Continuous Synthesis and Biological Screenings
• Application of ContinuousFlow Processing in Multistep API and Drug Syntheses
• ContinuousFlow Multistep Synthesis of Active Pharmaceutical Ingredients
• Enantioselective (Bio)Catalysis in Continuous Flow as Efficient Tool for the Synthesis of Advanced Intermediates and Active Pharmaceutical Ingredients
• Innovative Process Development of Pharmaceutical Intermediates Under ContinuousFlow System

The book editor Esther Alza was for many years the Manager of ERTFLOW at the Institute of Chemical Research of Catalonia ( ICIQ ), in Tarragona, Spain. Having obtained her PhD from ICIQ working on asymmetric catalysis and flow chemistry, she moved to the University of Cambridge as a Wellcome Trust Postdoctoral Fellow to work on medicinal chemistry. After this, she returned to ICIQ to lead the establishment of ERTFLOW as technology development unit. In 2020 she founded a spinoff that creates advanced technological tools for scientific research in the field of photochemistry, and recently she has also founded a company to develop further applications of flow microreactor technology in medicinal chemistry, process development, and novel technologies to offer this experience to pharmaceutical and fine chemistry companies.