ACS Combinatorial Science p. 365 - 374 (2011)
Update date:2022-08-03
Topics:
Gerard, Baudouin
Duvall, Jeremy R.
Lowe, Jason T.
Murillo, Tiffanie
Wei, Jingqiang
Akella, Lakshmi B.
Marcaurelle, Lisa A.
We have implemented an aldol-based "build/couple/pair" (B/C/P) strategy for the synthesis of stereochemically diverse 8-membered lactam and sultam scaffolds via SNAr cycloetherification. Each scaffold contains two handles, an amine and aryl bromide, for solid-phase diversification via N-capping and Pd-mediated cross coupling. A sparse matrix design strategy that achieves the dual objective of controlling physicochemical properties and selecting diverse library members was implemented. The production of two 8000-membered libraries is discussed including a full analysis of library purity and property distribution. Library diversity was evaluated in comparison to the Molecular Library Small Molecule Repository (MLSMR) through the use of a multifusion similarity (MFS) map and principal component analysis (PCA).
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Doi:10.1016/S0040-4020(01)89963-4
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