MACROCYCLIZATION REACTIONS AND INTERMEDIATE COMPOUNDS AND OTHER FRAGMENTS SUITABLE FOR PREPARING ANALOGUES OF HALICHONDRIN B Russian patent published in 2019 - IPC C07D493/22 C07D307/28 C07C6/02 

Abstract RU 2710545 C2

FIELD: chemistry.

SUBSTANCE: method involves conducting a macrocyclization reaction on a non-microcyclic intermediate compound, wherein said macrocyclization reaction provides said intermediate in preparing the eribulin by forming a C.15-C.16 bond in an eribulin structure, wherein said non-microcyclic intermediate compound is a compound of formula (IA) or salt thereof:

where value of radicals is given in the claim. Said intermediate in producing the eribulin is a compound of formula (IB) or salt thereof:

Macrocyclization reaction involves contacting a compound of formula (IA) or a salt thereof with an olefin metathesis catalyst. Also disclosed are embodiments of a method of producing an intermediate compound for producing eribulin, methods of producing eribulin or eribulin mesylate, methods of producing intermediate compounds and intermediate compounds.

EFFECT: present invention relates to a method of producing an intermediate compound for producing eribulin.

93 cl, 7 dwg, 10 ex

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RU 2 710 545 C2

Authors

Fan Frensis Dzh.

Kim Dae-Sik

Choj Khieong-Vook

Chejz Charlz I.

Li Dzaemoon

Dates

2019-12-27Published

2014-11-04Filed