Invention Grant
- Patent Title: Intermediates useful in the preparation of halichondrin compounds and methods for preparing the same
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Application No.: US16768943Application Date: 2019-11-07
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Publication No.: US11713329B2Publication Date: 2023-08-01
- Inventor: Weiping Xu
- Applicant: BEIJING TIENYI LUFU PHARMATECH CO. LTD.
- Applicant Address: CN Beijing
- Assignee: BEIJING TIENYI LUFU PHARMATECH CO. LTD.
- Current Assignee: BEIJING TIENYI LUFU PHARMATECH CO. LTD.
- Current Assignee Address: CN Beijing
- Agency: NKL Law
- Agent Allen Xue
- Priority: CN 1811508481.1 2018.12.10
- International Application: PCT/CN2019/116349 2019.11.07
- International Announcement: WO2020/119345A 2020.06.18
- Date entered country: 2020-06-02
- Main IPC: C07D263/26
- IPC: C07D263/26 ; C07F7/08 ; C07D277/16 ; C07D493/22 ; C07F7/18

Abstract:
The invention relates to intermediates useful in the preparation of halichondrin compounds, methods for preparing the same and use thereof, such as halichondrins, eribulin, or their analogs. The intermediates, the methods and use thereof are used for the synthesis of the C20-C26 fragment of halichondrin compounds. The raw materials in the synthetic route of the invention are cheap and easily obtained, the sources and the qualities of the raw materials are reliable. The choice of the methods useful in the synthesis of chiral central structures are based on the structural characteristics of the reactants, thus effectively improving the synthesis efficiency, reducing the difficulties and risks of product quality control, and avoiding the use of highly toxic and expensive organotin catalysts to significantly decrease costs and improve environmental friendliness.
Public/Granted literature
- US20210163509A1 Intermediates useful in the preparation of halichondrin compounds and methods for preparing the same Public/Granted day:2021-06-03
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