The invention discloses a method for chemically synthesising
gastrodin, comprising the following steps of: in the presence of a
molecular sieve, under the
catalysis of Lewis acid, and performing
glycosylation reaction on pent-acetyl-b-D-glucose and p-
cresol in an
organic solvent with to generate 4-methylphenyl-2,3,4,6-O-
tetra-acetyl-b-D-glucopyranoside; then preparing 4-halomethylphenyl-2,3,4,6-O-
tetra-acetyl-b-D-glucopyranoside from 4-methylphenyl-2,3,4,6-O-
tetra-acetyl-b-D-glucopyranoside and N-halosuccinimide in the presence of an initiator, and then reacting 4-halomethylphenyl-2,3,4,6-O-tetra-acetyl-b-D-glucopyranoside with the
mixed solution of glacial
acetic acid and
tertiary amine to obtain 4-acetoxylmethylphenyl-2,3,4,6-O-tetra-acetyl-b-D-glucopyranoside; and finally removing the acetyl
protecting group from the 4-acetoxylmethylphenyl-2,3,4,6-O-tetra-acetyl-b-D-glucopyranoside in an alkaline condition to obtain
gastrodin. Compared with the traditional method, the method disclosed by the invention has easily available raw materials, and is short in reaction time, capable of preparing the
reaction product in each step via recrystallization, simple, and more suitable for industrialized production for
gastrodin.