METHODS FOR SYNTHESIS OF HALICHONDRIN B ANALOGS Russian patent published in 2018 - IPC C07D493/22 

Abstract RU 2676486 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a method for producing an intermediate product for the synthesis of eribulin. Method comprises reacting a compound of formula (I) (I), where each of R1, R2, R3, R4 and R5 independently denotes a silyl group, with a fluoride source in an amide-containing solvent, to obtain intermediate product ER-811475 ER-811475. Amide is N,N-(C1-C6 dialkyl)C1-C6 alkylamide or N-(C1-C6 alkyl)C2-C6 lactam. Methods for producing an intermediate product for the synthesis of eribulin, methods for producing eribulin, and a method for producing a pharmaceutical product are also disclosed.

EFFECT: invention allows to obtain an intermediate product with a high degree of selectivity and increases the efficiency of the process for obtaining eribulin as a whole.

31 cl

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RU 2 676 486 C1

Authors

Lyuis Brajan M.

Khu Yunbo

Chzhan Khojmin

Tiba Khiroyuki

Komatsu Yuki

Dates

2018-12-29Published

2014-12-05Filed