Application of divergent multi-component reactions in the synthesis of a library of peptidomimetics based on γ-amino-α,β-cyclopropyl acids |
| |
Authors: | Peter Wipf Stefan Werner Grace H.C. Woo Corey R.J. Stephenson Maciej A.A. Walczak Claire M. Coleman Leslie A. Twining |
| |
Affiliation: | Center for Chemical Methodologies and Library Development (UPCMLD), University of Pittsburgh, Pittsburgh, PA 15260, USA |
| |
Abstract: | The multi-component condensation of organozirconocene, aldimine and zinc carbenoid was applied to the stereoselective synthesis of cyclopropane amino acid derivatives. These compounds served as scaffolds for the preparation of a 46-member library. The C- and N-termini of the cyclopropane amino acid derivatives were diversified by condensations with ten amines and ten acylating agents, respectively. To improve yields and accelerate library synthesis, most products were prepared under microwave irradiation and purified by polymer-bound scavengers and SPE methodology. All compounds were analyzed by LC-MS and a representative selection was fully characterized. |
| |
Keywords: | Indexed library Microwave irradiation Polymer-bound scavengers |
本文献已被 ScienceDirect 等数据库收录! |