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Updated: Jul 3, 2026

Synthesis of Information-bearing Peptoids and their Sequence-directed Dynamic Covalent Self-assembly
Published on: February 6, 2020
Synthetic studies on Et-743. Assembly of the pentacyclic core and a formal total synthesis
Dan Fishlock1, Robert M Williams
1Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
Abstract:
A formal total synthesis of the potent anticancer agent Et-743 is described. The tetrahydroisoquinoline core is stereoselectively constructed using a novel radical cyclization of a glyoxalimine. Further elaboration of this core rapidly accessed the pentacyclic core of Et-743, but a mixture of regiosisomers was obtained in the key Pictet-Spengler ring closure. A known advanced intermediate in the synthesis of Et-743 was intercepted, constituting a formal synthesis of the molecule.
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