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Total Synthesis of Tetrodotoxin.

Authors :
Murakami K
Toma T
Fukuyama T
Yokoshima S
Source :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2020 Apr 06; Vol. 59 (15), pp. 6253-6257. Date of Electronic Publication: 2020 Feb 19.
Publication Year :
2020

Abstract

A total synthesis of tetrodotoxin was accomplished. A Diels-Alder reaction between a known enone and a siloxy diene gave a tricyclic product, the steric bias of which was used to construct the remaining stereogenic centers. A nitrogen atom was introduced either by a four-step sequence involving a Curtius rearrangement, or a three-step sequence featuring a newly developed transformation of a terminal alkyne into a nitrile. Introduction of the guanidine moiety followed by the formation of the heterocyclic system by cascade reactions led to tetrodotoxin.<br /> (© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Details

Language :
English
ISSN :
1521-3773
Volume :
59
Issue :
15
Database :
MEDLINE
Journal :
Angewandte Chemie (International ed. in English)
Publication Type :
Academic Journal
Accession number :
31985136
Full Text :
https://doi.org/10.1002/anie.201916611