Industrial production method of Alogliptin benzoate

Abstract

The invention relates to an industrial production method of Alogliptin benzoate, and belongs to the technical field of industrial pharmacy. The method comprises three steps of 1, preparing an Alogliptin intermediate AG I; 2, preparing an Alogliptin intermediate AG II; 3, preparing the Alogliptin benzoate. The industrial production method has the beneficial effects that the reaction conditions areproper; the operation is simple and convenient; the realization is easy; only the Alogliptin intermediate AG II is prepared; then, the AG II and benzoic acid are subjected to tetrahydrofuran synthesis; the Alogliptin benzoate can be obtained; the process is saved; the cost is reduced; used solvents have small environment pollution; the operation is safe; under the large-scale industrial productioncondition, the existing average yield is only about 30 percent; under the condition that the final yield reaches 19.32kg, the finial product yield reaches 94.77 percent; the total yield reaches 60.11percent; high quality and purity can be maintained; the production efficiency is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of industrial pharmacy, in particular to an industrial production method of alogliptin benzoate. Background technique [0002] Alogliptin benzoate, chemical name: 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2 ,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile benzoate, its form is white or off-white crystalline powder. Soluble in dimethyl sulfoxide, soluble in methanol, slightly soluble in water, slightly soluble in ethanol. Its molecular formula is: C 18 h 21 N 5 o 2 .C 7 h 6 o 2 , Molecular weight: 461.51. The chemical structure is as follows. [0003] . [0004] Alogliptin benzoate is a highly selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-IV), maintaining glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide in vivo (GIP) levels, promote the secretion of insulin, thereby exerting a hypoglycemic effect. [0005] For the industriali...

AI Technical Summary

Problems solved by technology

Although the patent claims to be an industrialized production method, it is actually produced in small doses of grams or milliliters, and the steps are many and complicated. Although the yield of each step is 90.0%, 80.1%, and 70.5%. , 82.2%; when the final output is only 168 grams, the yield of the final product is only 82.2%, and the total yield is only 41.78%, which is still not high

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