The invention discloses a preparation method of
voglibose, which comprises the following steps: by taking
validamycin which is low in price and easy to obtain as a
raw material, hydrolyzing and removing impurities to obtain validinol A, splitting C-N bonds of the validinol A to form a mixture of two quasi-six-membered amino sugars which are difficult to separate, and separating the two quasi-six-membered amino sugars to obtain the
voglibose. The preparation method comprises the following steps: carrying out
intramolecular cyclization on a
selenium reagent loaded by a
high polymer and pseudo-six-membered
amino sugar (Va) containing double bonds to form a rigid
lactone compound, and immobilizing the rigid
lactone compound on resin through a carbon-
selenium bond to form resin (VI); according to the
process design, the problem of
stereoselectivity during synthesis of the key intermediate validalylamine is solved, and separation of two quasi-six-membered amino sugars (Va) and (Vb) is realized, namely, the precursor quasi-six-membered amino sugars (Vb) of the validalylamine (XI) are separated through simple filtering and washing operations;
cutting the resin (VI) through
sodium borohydride, hydrolyzing, carrying out
dehydration condensation on the resin (VI) and 1, 3-
dihydroxyacetone, and hydrogenating to obtain
voglibose; the method is short in
route and low in cost. # imgabs0 #