Synthetic Study of Kosinostatin Aglycon: Synthesis of the ABCDEFG Ring Skeleton
Open Access
- 18 June 2025
- journal article
- Published by American Chemical Society (ACS) in The Journal of Organic Chemistry
- Vol. 90 (26) , 9291-9294
Abstract
A synthetic method for the CDEFG substructure of kosinostatin was developed using the cyclization of the di-para-nosyl 3-(2-hydroxyethyl)pyrrolidin-2-imine derivative. The key to the success of this cyclization was the choice of the para-nosyloxy (p-NsO) group as the leaving group. This selection enabled the cyclization to proceed under mild reaction conditions, leading to the first construction of a kosinostatin-type scaffold. The method was further applied to the synthesis of the ABCDEFG ring of kosinostatin aglycon.Keywords
Funding Information
- Japan Society for the Promotion of Science (20H02744, 21K18964, 24K01490)
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