Total synthesis of TAK-kinase inhibitor LL-Z1640-2 via consecutive macrocyclization and transannular aromatization |
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| Authors: | Miyatake-Ondozabal Hideki Barrett Anthony G M |
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| Affiliation: | Department of Chemistry, Imperial College, London SW7 2AZ, England. |
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| Abstract: | The biomimetic total synthesis of LL-Z1640-2 (3) is reported without the use of phenol protection. The aromatic unit was constructed via the transannular aromatization of macrocyclic triketo-ester 2, which in turn was synthesized by macrolactonization using an intramolecular trapping of a triketo-ketene derived from dioxinone 1. |
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