Premium
The Generation of a Library of Bromodomain‐Containing Protein Modulators Expedited by Continuous Flow Synthesis
Author(s) -
Filipponi Paolo,
Baxendale Ian R.
Publication year - 2016
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201600222
Subject(s) - bromodomain , chemistry , continuous flow , flow chemistry , combinatorial chemistry , flow (mathematics) , nanotechnology , biochemical engineering , engineering , biochemistry , dna , materials science , geometry , mathematics , histone
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.