1356600-58-2Relevant academic research and scientific papers
Build/couple/pair strategy for the synthesis of stereochemically diverse macrolactams via head-to-tail cyclization
Fitzgerald, Mark E.,Mulrooney, Carol A.,Duvall, Jeremy R.,Wei, Jingqiang,Suh, Byung-Chul,Akella, Lakshmi B.,Vrcic, Anita,Marcaurelle, Lisa A.
, p. 89 - 96 (2012/04/11)
A build/couple/pair (B/C/P) strategy was employed to generate a library of 7936 stereochemically diverse 12-membered macrolactams. All 8 stereoisomers of a common linear amine precursor were elaborated to form the corresponding 8 stereoisomers of two regioisomeric macrocyclic scaffolds via head-to-tail cyclization. Subsequently, these 16 scaffolds were further diversified via capping of two amine functionalities on SynPhase Lanterns. Reagents used for solid-phase diversification were selected using a sparse matrix design strategy with the aim of maximizing coverage of chemical space while adhering to a preset range of physicochemical properties.
