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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 |
| Volume | 14 |
| Issue | 2 |
| Pages | 89-96 |
| Date Published (YYYY/MM/DD) | 2012/02/13 |
| ISSN Number | 2156-8952 |
| DOI | 10.1021/co200161z |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/22252910?dopt=Abstract |
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