The invention discloses a preparation method of L-echinacea A and an
acid salt thereof. The preparation method of the L-echinacea A
acid salt comprises the following synthetic
route. And carrying out
alkalization treatment on the L-inclusion canine A
acid salt, so as to obtain the L-inclusion canine. According to the invention,
pyridinium salt and chiral N-acryloyl oxazolidinone are taken as initial raw materials, a (2R, 5R, 6S) core skeleton of the obtuseline A is selectively constructed through a 1, 3-dipolar
cycloaddition reaction, then introduction of all carbon atoms in the obtuseline A is completed through processes of hydrogenation reduction,
transamination,
hydroboration reduction reaction,
methylation and the like, and the novel preparation method of the obtuseline A is realized. The preparation method comprises the following steps: by taking L-echinokimene as a
raw material, carrying out protection group replacement, oxidation
rearrangement reaction, protection group removal and other processes to prepare L-echinokimene acid salt, and carrying out
alkalization treatment on the L-echinokimene acid salt to obtain the L-echinokimene with optical activity, the whole
route is simple and convenient, the yield is good, the selectivity is relatively good, and the
reaction conditions are mild and controllable.