AI Article Synopsis
- A build/couple/pair (B/C/P) strategy was used to create a library of 7936 different 12-membered macrolactams.
- All 8 stereoisomers of a linear amine precursor were transformed into 16 macrocyclic scaffolds through head-to-tail cyclization.
- These scaffolds were then diversified further by capping amine functionalities using a targeted reagent selection approach to cover a wide range of chemical variations.
Article 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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3289975 | PMC |
| http://dx.doi.org/10.1021/co200161z | DOI Listing |
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