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Title:
CAMPTOTHECIN DERIVATIVE INTERMEDIATE AND SYNTHESIS METHOD THEREFOR, AND METHOD FOR SYNTHESIZING CAMPTOTHECIN DERIVATIVE BY USING INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2023/025138
Kind Code:
A1
Abstract:
Disclosed are novel exatecan mesylate intermediates 5 and A, and a preparation method for exatecan mesylate. Raw materials in the preparation method are cheap and easy to obtain, the synthetic route of the intermediate is simple, the "one-pot" reaction of oximation, catalytic hydrogenolysis and amino protection is avoided, the reaction steps are greatly reduced, the operation conditions are mild, the operation difficulty is reduced, the energy consumption is low, and the present invention is suitable for industrial scale-up production; the atom utilization is improved, and industrial application of green chemistry is better met; the yield of synthesis of an exatecan derivative is increased, and the cost is further reduced.

Inventors:
ZHENG JUNHAO (CN)
YU ZHEJIAN (CN)
ZHOU JING (CN)
Application Number:
PCT/CN2022/114203
Publication Date:
March 02, 2023
Filing Date:
August 23, 2022
Export Citation:
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Assignee:
HANGZHOU ZHONGMEIHUADONG PHARMACEUTICAL CO LTD (CN)
International Classes:
C07C231/12; C07C233/43; C07C233/54; C07C303/32; C07C309/04; C07D491/22
Domestic Patent References:
WO2020051435A12020-03-12
WO1998033762A11998-08-06
Foreign References:
CN111065621A2020-04-24
CN1276782A2000-12-13
EP0495432A11992-07-22
CN1175943A1998-03-11
CN111470998A2020-07-31
Attorney, Agent or Firm:
BEIJING LINKTEC IP LAW FIRM (SPECIAL GENERAL PARTNERSHIP) (CN)
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