This invention relates to a method for the direct synthesis of Aramchol from
cholic acid, belonging to the field of
organic synthesis technology. The key technical point of this invention is the method for the direct synthesis of Aramchol from
cholic acid. First, eicosanoyl
chloride is prepared from
arachidic acid and
thionyl chloride. Then, eicosanoamide is prepared from eicosanoyl
chloride and
ammonia-
methanol solution. The eicosanoamide is added to
tetrahydrofuran, followed by the addition of
cholic acid, diethyl azodicarbonate, and
triphenylphosphine. Aramchol is synthesized under the action of diethyl azodicarbonate and
triphenylphosphine. This method overcomes the shortcomings of existing techniques for synthesizing Aramchol from cholic acid, such as excessively long reaction routes, large consumption of
sodium azide and eicosanoyl chloride, complex side reactions, and poor reproducibility. The preparation method involves reactions at
room temperature, is simple to operate, has short steps, convenient post-
processing, and high yield, making it suitable for industrial application.