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Studies toward the total synthesis of microsclerodermin G

Date

2010

Authors

Burnett, Cameron Moeller, author
Williams, Robert Michael, advisor
Kennan, Alan J., committee member
Rovis, Tomislav, 1968-, committee member
Bernstein, E. R. (Elliot R.), committee member
Belisle, John Theodore, committee member

Journal Title

Journal ISSN

Volume Title

Abstract

We report our studies toward the synthesis of microsclerodermin G, a cyclic hexapeptide with antifungal and antitumor activity. The dehydrotryptophan amino acid was synthesized according to literature precedents. (3R)-γ-amino-β-hydroxybutyric acid (GABOB) was synthesized according to previous methodology from our research group. An aspartate-based precursor to the pyrrolidinone moiety of microsclerodermin G was prepared in four steps from known materials. 3-amino-6-methyl-12-phenyl-2,4,5-trihydroxydodeca-7,9,11-trienoic acid (AMPTD) was prepared in seven steps from known materials; the synthesis utilized Evans' chiral oxazolidinone glycolate aldol reaction and the sulfinimine-based Mannich reaction developed by Ellman. Syntheses of two dipeptides are reported, as are other attempts at coupling of the various amino acids.

Description

Department Head: Ellen R. Fisher.

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Subject

synthesis
AMPTD
microsclerodermin G
organic
Macrocyclic compounds -- Synthesis
Peptides -- Synthesis
Amino acids -- Synthesis

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