New Drug Approvals

Home » SPOTLIGHT » Flow chemistry approaches directed at improving chemical synthesis

Flow chemistry approaches directed at improving chemical synthesis



Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 


Blog Stats

  • 2,896,896 hits

Enter your email address to follow this blog and receive notifications of new posts by email.

Join 2,489 other followers

add to any



Flow synthesis offers many advantages when applied to the processing of difficult or dangerous chemical transformations. Furthermore, continuous production allows for rapid scale up of reactions without significant redevelopment of the routes. Importantly, it can also provide a versatile platform from which to build integrated multi-step transformations, delivering more advanced chemical architectures. The construction of multi-purpose micro and meso flow systems, that utilize in-line purification and diagnostic capabilities, creates a scenario of seamless connectivity between sequential steps of a longer chemical sequence. In this mini perspective, we will discuss our experience of target orientated multi-step synthesis as presented at the recent inaugural meeting of LEGOMEDIC at Namar University, Belgium.

The true potential of flow chemistry as an enabling technology can really only be fully appreciated when seen in the context of a target driven multi-step synthesis, aimed at the delivery of advanced chemical structures such as active pharmaceutical ingredients (APIs) .

As most pharmaceutical syntheses typically require between 8 and 10 chemical transformations (this is often somewhat reduced to 5/6 steps when analogue/library syntheses are being conducted), excluding protecting group manipulations, to realize the target molecule, this is a good foundation from which to explore the advantages of flow chemistry. We have generated a flow protocol for the synthesis of imatinib, the API of the Novartis block buster anticancer therapeutic Gleevec (imatinib mesylate), including a series of analogues (Scheme 11)

Furthermore, we aimed to create a route which would allow each of the three main fragments to be exchanged to address maximum variation in subsequent analogue synthesis. This requires additional planning to build flexibility into the sequence where this desired diversity can be easily introduced. Again, prior consideration of the generated intermediates, and any potential by-products that may arise, is critical and should be addressed prior to embarking on the synthesis.

Consequently, the extensive profiling of the reaction in terms of its purity profile is more closely analogous to process chemistry than traditional Medicinal Chemistry, even at the development stage. So, although more time consuming in the planning stage, having a greater understanding of the chemistry, does then enable a smoother up scaling and more rapid optimization of the route.

Scheme 11Flow route used to prepare imatinib related analogues.

read all this at

Flow chemistry approaches directed at improving chemical synthesis

Ian R. Baxendale1 / Laurens Brocken1 / Carl J. Mallia1

1Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK

Corresponding author: Ian R. Baxendale, Department of Chemistry, Durham University, South Road, Durham, DH1 3LE, UK

Citation Information: Green Processing and Synthesis. Volume 2, Issue 3, Pages 211–230, ISSN (Online) 2191-9550, ISSN (Print) 2191-9542, DOI: 10.1515/gps-2013-0029, May 2013


1 Comment

Leave a Reply

Fill in your details below or click an icon to log in: Logo

You are commenting using your account. Log Out /  Change )

Google photo

You are commenting using your Google account. Log Out /  Change )

Twitter picture

You are commenting using your Twitter account. Log Out /  Change )

Facebook photo

You are commenting using your Facebook account. Log Out /  Change )

Connecting to %s

This site uses Akismet to reduce spam. Learn how your comment data is processed.


Follow New Drug Approvals on

Enter your email address to follow this blog and receive notifications of new posts by email.

Join 2,489 other followers



DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with GLENMARK PHARMACEUTICALS LTD, Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 30 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, Dr T.V. Radhakrishnan and Dr B. K. Kulkarni, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 30 year tenure till date Dec 2017, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 9 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 50 Lakh plus views on dozen plus blogs, He makes himself available to all, contact him on +91 9323115463, email, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 19 lakh plus views on New Drug Approvals Blog in 216 countries...... , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc

Personal Links

View Full Profile →


Follow my blog with Bloglovin The title of your home page You could put your verification ID in a comment Or, in its own meta tag Or, as one of your keywords Your content is here. The verification ID will NOT be detected if you put it here.
%d bloggers like this: