A kind of preparation method of 3-o-carbamoylmannose donor derivative, bleomycin disaccharide and its precursor

A technology for carbamoyl mannose and derivatives, which is applied in the field of medicine and chemical industry, can solve the problems of difficult purification, poor sorbitol selectivity, slow progress and the like, and achieves the effects of strong operability, cheap raw materials and high selectivity
CN108794547BActive Publication Date: 2021-08-10GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
Publication Date
2021-08-10

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Abstract

The invention discloses a preparation method of 3-O-carbamoylmannose donor derivatives, which comprises selective benzylation, acetylation, debenzylation and aminomethylation of the 3-hydroxyl group of methyl-α-mannoside Acylation series reaction. At the same time, the invention also discloses a method for preparing bleomycin disaccharide and its precursor by using the 3-O-carbamoylmannose donor derivative prepared by the method as a donor. The preparation method of the 3‑O‑carbamoylmannose donor derivative of the present invention has the advantages of high protection and deprotection selectivity, short route and high yield, and simultaneously solves the problem of the production of bleomycin disaccharide and its precursor. Low efficiency, poor operability and repeatability of the reaction, unsuitable for industrialization and other problems, has the advantages of cheap and easy-to-obtain raw materials, high yield, strong operability, easy control of conditions, industrial scale-up, high efficiency and low cost.
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Description

technical field

[0001] The invention belongs to the technical field of medicine and chemical industry, and in particular relates to a preparation method of a 3-O-carbamoylmannose donor derivative, bleomycin disaccharide and its precursor. Background technique

[0002] Bleomycin (BLM) is a glycopeptide antitumor antibiotic drug used in the first-line clinical treatment of tumors. It is mainly used to treat squamous cell carcinoma, Hodgkin's malignant lymphoma, cervical cancer and testicular cancer. Streptomyces verticillus. The BLM structure consists of three parts: 1) 5 amino acids composed of pyrimidine-imidazole structure; 2) 1 side chain containing bithiazole amino group; 3) 1 unique disaccharide structure. A large number of studies have shown that the pyrimidine-imidazole structure is the key part of the anti-tumor effect of BLM, which can selectively oxidize and cleave the 5'-GC-3' and 5'-GT-3' sequences in DNA, thereby exerting anti-tumor activity; The structure can ...

Claims

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