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especially in the screening of reaction have a prominent role. Kulkarni et al. of tBuOK as a base into a 10 mL reac- either avoided by utilizing the carba- in the absence of a solvent with an over- chemicals, APIs, intermediates, KSMs
parameters to fi nd the optimal conditions. (OPRD, 2012) and Reddy et al. (2013, tor coil at 100°C with a residence time mate in the ring closure or integrated all yield of 90% and an output of 2.4 g/h. and also some important natural pro-
17, 10, 1272-1276)) have demonstrated of 20 min. Suzuki Coupling is done in within an in-line purifi cation; and (iii) (Porta, R.; Benaglia, M.; Puglisi, A., ducts has become a reality and Indian
In a similar manner, a safe and rap- the effi cacy of using fl ow synthesis for a fi xed bed reactor. (Porta, et al., Org. this is the fi rst integrated, continuous- Org. Process Res. Dev. 2016, 20, 1, academia as well as industry must latch
id method for the synthesis of α-nitro controlled sulfoxidation for the synthe- Process Res. Dev. 2016, 20, 1, 2-25). fl ow preparation of an aryl piperazine 2-25). Advantages over batch process on to this. The tremendous progress being
esters has been reported by Chentosva et sis of benzimidazole core drugs, such Advantages over batch process include: CNS drug. include: (i) overall yield > 90%; (ii) an witnessed in CROs and CDMOs in
al. (J. Org. Chem. 2016, 81, 19, 9415- as ismaprazole, lansoprazole, pantapra- (i) no requirement of any intermediate output of 2.4 g/h at the lab scale; and India in this direction is quite encour-
9421) via the trapping of nitronium ions. zole, and rabeprazole. The approach purifi cation or solvent switching; and Lesinurad (iii) solvent-free greener method. aging. However, it needs to multiply
The two-stage nitration and subsequent has helped reduce the reaction time (ii) fully automated process reduces It is an URAT1 inhibitor in which and become an integral part of process
deacetylation of readily available 1,3- from several hours to few minutes. waste and unit operations. telescoped s-alkylation of thiol deriva- At CSIR-National Chemical Labo- development.
dicarbonyl compounds was achieved tive with ethyl chloroacetate to gene- ratory, Pune, we have also developed
Expo & Conference News
using a biphasic semi-continuous Alkylation reactions Flibanserin rate 3-thio-1,2,4-triazole in 91% overall many CFS methods over last 15 years. Trained manpower that understands
approach. α-Nitro esters and amides Some alkylation reactions, reported It is a medication used to treat hypo- yield. (Damião, et al. React. Chem. Here in this article, we have tried to Green Chemistry and its implementa-
were obtained in good overall yields using CFS strategies for preparations active sexual desire disorder (HSDD) Eng., 2020, 5, 865-872). Advantages collect few important reaction types tion is also an essential factor for this
(53-84%). of some important drugs are described in premenopausal women. Greiner and over batch process include: (i) 68% including, fl uorination, chlorination, success. Academia must get away from
below. co-workers developed an interrupted overall yield in a total residence time of alkylation, Grignard reaction, nitration conventional synthesis mind-set and
Similarly, Köckinger et al. (Org. one-fl ow system for the synthesis of 2 hours; (ii) a fi ve-step linear continu- and diazotization that have been adapt to CFS as well as new paradigm
Process Res. Dev. 2020, 24, 10, Telemisartan fl ibanserin with less number of manual ous fl ow sequence; and (iii) fast gene- used for preparations of some useful of mechanochemistry.
2217-2227) have reported nitration of Telemisartan is the API present in unit operations. Previous existing batch ration of Lesinurad can be scaled-up molecules in pharmaceutical sector or
acetylated 4-fl uoro-2-methoxyaniline the antihypertensive drug, Micardis. It protocols to fl ibanserin included pro- seamlessly. as medicine. The need for greening the The decision of PLI Schemes in
producing 4-fl uoro-2-methoxy-5- is an angiotensin receptor antagonist. tecting group introduction and removal pharmaceutical sector must involve future must also consider green index
nitroaniline, which is an important inter- Gupton and co-workers developed a as separate steps, which was not con- Diphenhydramine hydrochloride checking its viability in continuous of a process, which should have clear
mediate for Osimertinib. The approach continuous fl ow convergent multi-step sidered feasible. Alternatively, reported Diphenhydramine hydrochloride is fl ow mode. criteria on why certain types of reac-
has specifi c advantages over batch synthesis of telemisartan, which did not N-alkylation were challenging and widely used in synthesis of many drugs. tions must be done only in continuous
process that clearly indicate a greener require any intermediate purifi cation required forcing reaction conditions Jamison and co-workers developed a CONCLUSIONS mode. Keeping energy effi ciency in
approach. It has resulted in 82% isolated or solvent switching. This fully auto- with insoluble bases (Bana, et al. Chem. continuous fl ow process for the synthe- Application of the fl ow techno- mind, only such decisions will help in
yield over two steps, corresponding to mated process represents a signifi cant Eng., 2019, 4, 652–657.). sis of Diphenhydramine hydrochloride logies for the preparation of fi ne long term sustainability.
able individuals driving innovation
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a throughput of 25 mmol/h at the lab improvement over traditional batch panediol to maximize performance’.
sector, including R&D professionals,
take attendees through a variety of
scale, 0.46 kg/h at the pilot scale and procedure since it reduces waste and Homing in on a key focus area for
Advantages over batch process
formulation techniques focusing on
scientists,
innovators, and
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