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

Filipponi, P.; Baxendale, I.R.

doi:10.1002/ejoc.201600222

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

Filipponi, P.; Baxendale, I.R.

Authors

P. Filipponi

Professor Ian Baxendale i.r.baxendale@durham.ac.uk
Professor

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.

Citation

Filipponi, P., & Baxendale, I. (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. https://doi.org/10.1002/ejoc.201600222

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

Files

Accepted Journal Article (674 Kb)
PDF

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.