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The Generation of a Library of ­Bromodomain-Containing Protein Modulators Expedited by Continuous Flow Synthesis

Filipponi, P.; Baxendale, I.R.

The Generation of a Library of ­Bromodomain-Containing Protein Modulators Expedited by Continuous Flow Synthesis Thumbnail


Authors

P. Filipponi



Abstract

A continuous flow process delivering key building blocks for a series of BCP modulator libraries is reported. A dynamically mixed flow reactor emerged as a pivotal technology in both synthesis and isolation phases enabling the processing of slurries and suspensions while maintaining high productivity and reliability. Accordingly, the synthesis of common intermediates in flow were employed to further build a pyridazone-based library (36 compounds) aimed at improving lead compound potency and selectivity while further enabling structure-activity relationship studies of a new BCP modulator family.

Journal Article Type Article
Acceptance Date Mar 21, 2016
Online Publication Date Mar 22, 2016
Publication Date Apr 1, 2016
Deposit Date Mar 22, 2016
Publicly Available Date Mar 22, 2017
Journal European Journal of Organic Chemistry
Print ISSN 1434-193X
Electronic ISSN 1099-0690
Publisher Wiley
Peer Reviewed Peer Reviewed
Volume 2016
Issue 11
Pages 2000-2012
DOI https://doi.org/10.1002/ejoc.201600222
Public URL https://durham-repository.worktribe.com/output/1408670

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Copyright Statement
This is the peer reviewed version of the following article: Filipponi, P. and Baxendale, I. R. (2016), The Generation of a Library of ­Bromodomain-Containing Protein Modulators Expedited by Continuous Flow Synthesis. European Journal of Organic Chemistry, 2016(11): 2000-2012, which has been published in final form at http://dx.doi.org/10.1002/ejoc.201600222. This article may be used for non-commercial purposes in accordance With Wiley-VCH Terms and Conditions for self-archiving.





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