Title:
INTERMEDIATES FOR PREPARING HALICHONDRIN COMPOUNDS AND PREPARATION METHOD THEREFOR
Document Type and Number:
WIPO Patent Application WO/2020/119345
Kind Code:
A1
Abstract:
The present invention relates to intermediates for preparing halichondrin compounds, preparation methods therefor and use thereof, and particularly to intermediates for preparing halichondrin, eribulin or analogues thereof, preparation methods therefor and use thereof. The intermediates, preparation method therefor and use thereof are used to construct C20-C26 structural fragments of halichondrin compounds. Starting materials of synthetic routes of the present invention are inexpensive and readily available, and have stable sources and reliable quality. The choice of a chiral center construction method takes full advantage of structural features of reactants themselves, and improves the synthesis efficiency and reduces the difficulty and risk of product quality control. In addition, the use of a highly toxic and expensive organotin catalyst is avoided, and the cost and environmental friendliness are significantly improved.
Inventors:
XU WEIPING (CN)
Application Number:
PCT/CN2019/116349
Publication Date:
June 18, 2020
Filing Date:
November 07, 2019
Export Citation:
Assignee:
BEIJING TIENYI LUFU PHARMATECH CO LTD (CN)
International Classes:
C07F7/18
Domestic Patent References:
| WO2016003975A1 | 2016-01-07 | |||
| WO1993017690A1 | 1993-09-16 | |||
| WO2016003975A1 | 2016-01-07 |
Foreign References:
| CN201811508481A | 2018-12-10 |
Other References:
UEDA, A. ET AL.: "Total Synthesis of Halichondrin A, the Missing Member in the Halichondrin Class of Natural Products", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 136, no. 13, 7 March 2014 (2014-03-07), pages 5171 - 5176, XP055251183, DOI: 10.1021/ja5013307
DONG, CHENGGUO ET AL.: "New Syntheses of E7389 C14-C35 and Halichondrin C14-C38 Building Blocks: Reductive Cyclization and Oxy-Michael Cyclization Approaches", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 131, no. 43, 10 June 2009 (2009-06-10), pages 15642 - 15646, XP055241185
ZHANG, ZHIGAO ET AL.: "Total Synthesis of (-)-Exiguolide", ORGANIC LETTERS, vol. 17, 15 September 2015 (2015-09-15), pages 4706 - 4709, XP055702063
See also references of EP 3686208A4
DONG, CHENGGUO ET AL.: "New Syntheses of E7389 C14-C35 and Halichondrin C14-C38 Building Blocks: Reductive Cyclization and Oxy-Michael Cyclization Approaches", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 131, no. 43, 10 June 2009 (2009-06-10), pages 15642 - 15646, XP055241185
ZHANG, ZHIGAO ET AL.: "Total Synthesis of (-)-Exiguolide", ORGANIC LETTERS, vol. 17, 15 September 2015 (2015-09-15), pages 4706 - 4709, XP055702063
See also references of EP 3686208A4
Attorney, Agent or Firm:
BEIJING ORIGINTELLIGENCE IP LAW FIRM (CN)
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