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Updated: Jul 20, 2026

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
Published on: June 20, 2014
Asymmetric, stereocontrolled total synthesis of paraherquamide A
Robert M Williams1, Jianhua Cao, Hidekazu Tsujishima
1Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA. rmw@chem.colostate.edu
Abstract:
The first total synthesis of paraherquamide A, a potent anthelmintic agent isolated from various Penicillium sp. with promising activity against drug-resistant intestinal parasites, is reported. Key steps in this asymmetric, stereocontrolled total synthesis include a new enantioselective synthesis of alpha-alkylated-beta-hydroxyproline derivatives to access the substituted proline nucleus and a highly diastereoselective intramolecular S(N)2' cyclization to generate the core bicyclo[2.2.2]diazaoctane ring system.
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