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

Filipponi, P.; Baxendale, I.R.

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
• Public URL: https://durham-repository.worktribe.com/output/1408670