Study On The Synthesis Of Alibendol

With the improvement of people's living standards and large change of diet, people's hepatobiliary diseases incidence increasing. Cholecystagogues is very important to the hepatobiliary disease patients. Alibendol, chemical name is 2-hydroxy-N-(2-hydroxyethyl)-3-methoxy-5-(2-propenyl)benzamide is known as antispasmodic, chleretic, and cholekinetic active pharmaceutical ingredient which is useful in treatment of dyspepsia due to biliary insufficiency, alimentary intolerance, urticaria, pruritus, migraine, and constipation of hepatic origin.The synthesis of alibendol were reported in this article. o-vanillin was used as the materials and methanol was used as solvent. With o-vanillin as the original raw materials in methanol solvent,Methyl 2-hydroxy-3-methoxybenzoate was synthesized via one-pot oxidative esterification method.Then, Methyl 2-hydroxy-3-methoxy-5-(2-propenyl)benzoate was prepared via allylation and Claisen rearrangement reaction by Methyl 2-hydroxy-3-methoxybenzoate and allyl bromide.The last step of synthesis of Alibendol was straight forward formation of the amide by the reaction of Methyl 2-hydroxy-3-methoxy-5-(2-propenyl)benzoate with ethanolamine at 120℃。1HNMR and IR spectral data were obtained.The effect of several conditions such as reaction time and temperature on yields were investigated we reported a facile synthesis of Alibendol from o-vanillin via one-pot oxidative esterification method, the work will provide Referential value for future.