64-86-8Relevant articles and documents
SEMISYNTHETIC PROCESS FOR THE PREPARATION OF COLCHICINE
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Page/Page column 11; 12, (2022/01/05)
The invention relates to a process for the preparation of colchicine 1 from colchicoside 2 which comprises enzymatic conversion of colchicoside 2 to 3-O- demethylcolchicine 3, wherein the enzyme used is a cellulase. According to another aspect of the invention, 3-O-demethylcolchicine 3 can be converted to colchicine 1 using an alkylating agent. The invention also relates to a process for enriching the colchicine 1 content of extracts from plants belonging to the Colchicaceae family containing colchicine 1, colchicoside 2 and 3 -(9-demethyl colchicine 3, which comprises conversion by means of a colchicoside 2 cellulase to 3-O-demethylcolchicine 3, followed by conversion of 3-O-demethylcolchicine 3 to colchicine 1 using an alkylating agent.
Asymmetric synthesis method of colchicine and allocolchicine
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Paragraph 0040; 0043; 0058; 0066-0067, (2020/04/17)
The invention provides an asymmetric synthesis method of colchicine and allocolchicine, and belongs to the field of chemical synthesis. According to the invention, cheap commercial isovanillin A is used as a raw material, asymmetric allyl amination catalyzed by metal Ir is taken as a key reaction, a cyclization precursor E is obtained through Suzuki coupling reaction with a halide D, allocolchicine F is rapidly synthesized through intramolecular oxidative coupling, and finally, efficient asymmetric synthesis of colchicine I is completed through a bionic cyclopropane ring-opening strategy. Thesynthesis strategy used in the invention is simple and economic, good in operability and short in time consumption, and can meet the requirements of new drug development and large-scale preparation.
Synthesis method of colchicine
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, (2017/11/04)
The invention relates to a synthesis method of colchicine. According to the synthesis method of the colchicine, a compound as shown in the specification is used as a raw material, and then efficient intramolecular [5+2] cycloaddition is considered as key reaction; in combination with locating group guided dehydrogenation Hike reaction and Walker reaction, a molecular skeleton structure is rapidly constructed, so that an obtained structural formula, which has the same structure as a natural product, is the colchicine; and a modification research can be carried out on the colchicine favorably, so as to improve the bioactivity and the toxic and side effects of the colchicine.