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Scalable synthesis of the C14–C23 fragment of Eribulin and Halichondrin B
Kim U Bin,Samala Srinivas,Kim Namhyeon,Bogonda Ganganna,Lago‐Santomé Hugo,Jeong Youngdo,Kim Jin,Jung Jaehun,Jeon Sung‐Hyun,Lee Seung Jong,신현석 대한화학회 2022 Bulletin of the Korean Chemical Society Vol.43 No.12
A novel, scalable approach to the C14–C23 fragment of eribulin mesylate is disclosed. Key 2,3-Wittig rearrangement is strategically effected via [Rh] mediated decomposition of 1,2,3-triazole intermediate to derive the 2,5-trans-tetrahydrofuran motif, enabling multi-kilogram access to the desired C14–C23 fragment.