scholarly journals Continuous Flow Synthesis of Anticancer Drugs

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6992
Author(s):  
Mara Di Filippo ◽  
Marcus Baumann

Continuous flow chemistry is by now an established and valued synthesis technology regularly exploited in academic and industrial laboratories to bring about the improved preparation of a variety of molecular structures. Benefits such as better heat and mass transfer, improved process control and safety, a small equipment footprint, as well as the ability to integrate in-line analysis and purification tools into telescoped sequences are often cited when comparing flow to analogous batch processes. In this short review, the latest developments regarding the exploitation of continuous flow protocols towards the synthesis of anticancer drugs are evaluated. Our efforts focus predominately on the period of 2016–2021 and highlight key case studies where either the final active pharmaceutical ingredient (API) or its building blocks were produced continuously. It is hoped that this manuscript will serve as a useful synopsis showcasing the impact of continuous flow chemistry towards the generation of important anticancer drugs.

Author(s):  
Victor R. L. J. Bloemendal ◽  
Bram Spierenburg ◽  
Thomas J. Boltje ◽  
Jan C. M. van Hest ◽  
Floris P. J. T. Rutjes

AbstractContinuous flow chemistry holds great potential for the production of biologically relevant molecules. Herein, we present an approach for the continuous synthesis of cannabidiol and tetrahydrocannabinol in a one-flow system. The designed route consists of a reaction cascade involving Friedel-Crafts alkylation, subsequent ring opening and cyclisation in up to 45% yield. The reactions were successfully performed using both hetero- and homogeneous Lewis acids in continuous flow and provide yields that are similar to comparable batch processes. Graphical abstract


Synthesis ◽  
2021 ◽  
Author(s):  
Marcus Baumann ◽  
Thomas S Moody ◽  
Megan Smyth ◽  
Scott Wharry

Continuous flow chemistry is becoming an established technology platform that finds frequent application in industrial chemical manufacture with support and endorsements by the FDA for pharmaceuticals. Amongst the various advantages that are commonly cited for flow chemistry over batch processing, sustainability continues to require further advances and joint efforts by chemists and chemical engineers in both academia and industry. This short review highlights developments within the last 5 years that positively impact on the green credentials associated with flow chemistry, specifically when applied to the preparation of pharmaceuticals. An industrial perspective on current challenges is provided to whet discussion and stimulate further investment towards achieving greener modern synthetic technologies.


2020 ◽  
Author(s):  
Tomas Hardwick ◽  
Rossana Cicala ◽  
Nisar Ahmed

<p>Many chiral compounds have become of great interest to the pharmaceutical industry as they possess various biological activities. Concurrently, the concept of “memory of chirality” has been proven as a powerful tool in asymmetric synthesis, while flow chemistry has begun its rise as a new enabling technology to add to the ever increasing arsenal of techniques available to the modern day chemist. Here, we have employed a new simple electrochemical microreactor design to oxidise an L-proline derivative at room temperature in continuous flow. Flow performed in microreactors offers up a number of benefits allowing reactions to be performed in a more convenient and safer manner, and even allow electrochemical reactions to take place without a supporting electrolyte due to a very short interelectrode distance. By the comparison of electrochemical oxidations in batch and flow we have found that continuous flow is able to outperform its batch counterpart, producing a good yield (71%) and a better enantiomeric excess (64%) than batch with a 98% conversion. We have, therefore, provided evidence that continuous flow chemistry has the potential to act as a new enabling technology to replace some aspects of conventional batch processes. </p>


Author(s):  
Nicole Candice Neyt ◽  
Darren Lyall Riley

The adoption of flow technology for the manufacture of chemical entities, and in particular pharmaceuticals, has seen rapid growth over the past two decades with the technology now blurring the...


2017 ◽  
Vol 7 (3–4) ◽  
pp. 157-158 ◽  
Author(s):  
Daniel Blanco-Ania ◽  
Floris P. J. T. Rutjes

ChemInform ◽  
2014 ◽  
Vol 45 (44) ◽  
pp. no-no
Author(s):  
Jan Hartwig ◽  
Jan B. Metternich ◽  
Nikzad Nikbin ◽  
Andreas Kirschning ◽  
Steven V. Ley

Author(s):  
Cloudius Sagandira ◽  
Sinazo Nqeketo ◽  
Kanysile Mhlana ◽  
Thembela Sonti ◽  
Paul Watts ◽  
...  

Continuous flow chemistry has opened a new paradigm in both the laboratory and pharmaceutical industry. This review details the recently reported literature on continuous multistep telescoped synthesis of active pharmaceutical...


Author(s):  
Jessica Orrego‐Hernández ◽  
Helen Hölzel ◽  
Maria Quant ◽  
Zhihang Wang ◽  
Kasper Moth‐Poulsen

2021 ◽  
pp. 145-178
Author(s):  
Kian Donnelly ◽  
Mara Di Filippo ◽  
Cormac Bracken ◽  
Marcus Baumann

Sign in / Sign up

Export Citation Format

Share Document