Method for preparing eribulin and intermediate thereof

A technology for compounds and analogs, applied in the field of preparation of eribulin, can solve problems such as difficulty in total synthesis, complex structure, etc., and achieve the effects of avoiding complex and tedious processes and improving yield
CN108341828AActive Publication Date: 2018-07-31JIANGSU HENGRUI MEDICINE CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JIANGSU HENGRUI MEDICINE CO LTD
Publication Date
2018-07-31

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Abstract

The present invention relates to a method for preparing eribulin and an intermediate thereof. In particular, the invention relates to a method for preparing a compound of formula 5, R3 is selected from aldehyde or OR1, n=0 or 1, R1 is a hydroxy protecting group, and preferably the hydroxy protecting group is selected from tert-butyldimethylsilyl, tert-butyldiphenylsilyl, p-methoxybenzyl or benzyl.The invention also provides a method for preparing halichondrin and derivatives thereof such as the eribulin from the compound of formula 5.
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Description

technical field

[0001] The present invention relates to a method for preparing eribulin and a preparation method of its intermediate compound of formula 5. Background technique

[0002] Halichondrin B (Halichondrin B) is a natural product with anti-tumor activity, which was originally isolated from the marine sponge black soft sponge. Eribulin is the first macrocyclic ketone analog obtained by optimizing the structure of halichondrin B. At present, Eribulin mesylate injection has been marketed in many countries for the treatment of metastatic breast cancer, but its structure is complex And it contains multiple chiral neutrals, and the total synthesis is difficult.

[0003]

[0004] Therefore, development of a synthetic method for preparing eribulin for use as an antitumor agent is required.

[0005] US6214865 and US5436238 reported the synthesis of halichondrin and its derivatives using compound 2,5-disubstituted (2S,5S)-3-methylene-tetrahydrofuran (compound of formula ...

Claims

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