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Updated: May 20, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
A "catch-react-release" method for the flow synthesis of 2-aminopyrimidines and preparation of the Imatinib base
Richard J Ingham1, Elena Riva, Nikzad Nikbin
1Innovative Technology Centre, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK.
Abstract:
The development of a monolith-supported synthetic procedure is reported, taking advantage of flow processing and the superior flow characteristics of monolithic reagents over gel-phase beads, to allow facile access to an important family of 2-aminopyrimidine derivatives. The process has been successfully applied to a key precursor on route to Imatinib (Ar = 3-pyridyl, R(1) = 2-methyl-5-nitrobenzyl, R(2) = H).
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