The Story of Gefapixant Citrate (9): Flow Chemistr...

Org. Process Res. Dev. 2020, 24, 2478. DOI: 10.1021/acs.oprd.0c00252

◆The requirement for a greater excess of EF and KOt-Bu in the batch−batch process was attributed to the unproductive consumption of EF by KOt-Bu

◆The team developed a flow process leading to a significantly greener process. As an added benefit, the newly developed flow−batch process is more robust and can tolerate a wide range of conditions

◆Using less EF and KOt-Bu ensured less alkoxide was left in the solution at the end of formylation and that guanidine was less likely to be converted to biguanide and, ultimately, triazine byproduct (5). The number of equivalents of KOt-Bu required to drive the reaction to completion was decreased from 2.25 to 1.4 (a 38% reduction), the number of equivalents of EF from 2.0 to 1.3 (a 35% reduction), and the number of equivalents of G·HCl from 8.0 to 4.0 (a 50% reduction).

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