MACROCYCLISATION REACTION AND INTERMEDIATE COMPOUND AND OTHER FRAGMENTS, USEFUL IN SYNTHESIS OF MACROLIDES OF HALICHONDRINS Russian patent published in 2020 - IPC C07D407/14 C07D493/22 

Abstract RU 2739034 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to methods of producing macrocyclic intermediate compounds for synthesis of macrolides of halichondrins, which include subjecting a non-microcyclic compound of a carbon-carbon bond formation reaction (olefination reaction (e.g. Horner—Wadsworth—Emmons olefination reaction), catalytic metathesis of olefins with closing a cycle or a Nozaki—Hiyama—Kishi reaction) to obtain a macrocyclic macrolide. Invention also relates to intermediate compounds which find application as intermediate compounds in synthesis of macrolides of halichondrins, and methods of producing macrolide halichondrin, which is used in medicine as an anticancer agent.

EFFECT: disclosed are macrocyclization reactions and an intermediate compound and other fragments useful in the synthesis of macrolides of halichondrins.

53 cl, 7 dwg, 8 ex

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RU 2 739 034 C2

Authors

Fang, Francis, G.

Chase, Charles, E.

Kim, Dae-Shik

Choi, Hyeong-Wook

Dates

2020-12-21Published

2016-05-09Filed