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Build/Couple/Pair Strategy for the Synthesis of Stereochemically Diverse Macrolactams via Head-to-Tail Cyclization.
|Publication Type||Journal Article|
|Authors||Fitzgerald, ME, Mulrooney CA, Duvall JR, Wei J., Suh BC, Akella LB, Vrcic A., and Marcaurelle LA|
|Abstract||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.|
|Year of Publication||2012|
|Journal||ACS combinatorial science|
|Date Published (YYYY/MM/DD)||2012/02/13|