PYRAN FUSED RING COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF

Title:

PYRAN FUSED RING COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2019/166019

Kind Code:

A1

Abstract:

Disclosed in the present invention are pyran fused ring compounds, preparation methods therefor and the use thereof, in particular pyran fused ring compounds which can be used for preparing halichondrin, eribulin or analogues thereof, preparation methods therefor and the use thereof. Use of any one of the compounds of formulas (I) to (XIII) of the invention in the preparation of halichondrin B, eribulin, analogues thereof or C1-C13 moieties thereof. The present invention provides intermediates for the synthesis of halichondrin B, eribulin, or analogues thereof, in particular key products of C1-C13 moieties thereof, preparation methods therefor and the use thereof. The starting materials for the synthetic routes of the present invention are inexpensive, come from a stable source and have reliable quality. The selection of a chiral center construction method makes full use of the structural characteristics of reactants themselves, effectively improves the synthesis efficiency and reduces the difficulty and risk in product quality control. The use of highly toxic and expensive, high valence osmium catalysts is avoided, significantly improving cost and environmental friendliness.

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Inventors:

XU WEIPING (CN)

Application Number:

PCT/CN2019/076757

Publication Date:

September 06, 2019

Filing Date:

March 01, 2019

Export Citation:

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Assignee:

BEIJING TIENYI LUFU PHARMATECH CO LTD (CN)

International Classes:

C07D493/04; A61K31/335; A61P35/00; C07D309/10

Domestic Patent References:

WO2018006031A1	2018-01-04
WO2017168309A1	2017-10-05

Foreign References:

CN1993342A

2007-07-04

Other References: