75281-54-8Relevant academic research and scientific papers
Preparation method of edoxaban intermediate
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, (2018/04/03)
The invention discloses a preparation method of edoxaban intermediate (1S, 3R, 4R)-3-tert-butoxycarbonylamino-4-hydroxy-cyclohexanecarboxylic acid. According to the preparation method, 3-amino-4-hydroxy-cyclohexane carboxylate represented by formula IV is taken as a raw material, protective reaction with amino protection groups is carried out so as to obtain 3-tert-butoxycarbonylamino-4-hydroxy-cyclohexane carboxylate represented by formula V, enzyme catalyzed esterification resolution reaction is carried out so as to obtain optically pure (1S, 3R, 4R)-3-tert-butoxycarbonylamino-4-hydroxy-cyclohexane carboxylate represented by formula VII, and at last lithium hydroxide hydrolysis is adopted so as to obtain the (1S, 3R, 4R)-3-tert-butoxycarbonylamino-4-hydroxy-cyclohexanecarboxylic acid represented by formula VI. The preparation method possesses following advantages: operation is simple, the preparation method is green, is friendly to the environment, and is high in selectivity and lowin cost, large scale industrialized production can be realized, and it is convenient for industrial popularization.
