A “Catch–React–Release” Method for the Flow Synthesis of 2-Aminopyrimidines and Preparation of the Imatinib Base

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 success...

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Bibliographic Details
Published in:Organic letters 2012-08, Vol.14 (15), p.3920-3923
Main Authors: Ingham, Richard J, Riva, Elena, Nikbin, Nikzad, Baxendale, Ian R, Ley, Steven V
Format: Article
Language:English
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Summary: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, R1 = 2-methyl-5-nitrobenzyl, R2 = H).
ISSN:1523-7060
1523-7052
DOI:10.1021/ol301673q