Build/Couple/Pair Strategy for the Synthesis of Stereochemically Diverse Macrolactams via Head-to-Tail Cyclization
ACS Combinatorial Science2012Vol. 14(2), pp. 89–96
Citations Over TimeTop 10% of 2012 papers
Mark E. Fitzgerald, Carol A. Mulrooney, Jeremy R. Duvall, Jingqiang Wei, Byung‐Chul Suh, Lakshmi B. Akella, Anita Vrcic, Lisa A. Marcaurelle
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.
Related Papers
- → Effect of Folin Reagent from Different Sources on Protease Determination(2013)1 cited
- → Fluorinated Organocopper Reagents(2011)1 cited
- → A New Reagent for the Decoloration and Deproteinization of Urine for the Polarimetric Determination of Glucose(1962)1 cited
- STUDIES ON ANALYTICAL FUNCTIONAL GROUPS OF ORGANIC REAGENTS USED IN INORGANIC ANALYSIS——II.ON REAGENTS FOR ANTIMONOUS IONS(1956)
- Performance evaluation of stability of the total bile acid reagent with improved reagent bottles(2011)