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Synthesis process of alogliptin benzoate

A synthesis process, the technology of benzoic acid, which is applied in the field of diabetes treatment, can solve the problems of cumbersome post-processing, high cost of raw materials, complicated operation, etc., and achieve the effect of improving purity, reducing synthesis cost and simplifying synthesis process

Inactive Publication Date: 2021-02-09
重庆化工职业学院
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The object of the present invention is to provide a kind of synthesis technique of alogliptin benzoate, possess the synthetic route raw material cheap and easy to get, reduce the cost of synthesis, and each step is a classic reaction, easy to improve synthetically; Process raw material cost after improvement The advantages of low cost, simple operation, mild reaction conditions, simple post-treatment, and suitable for industrial production solve the problems of high raw material cost, complicated operation and cumbersome post-treatment in the existing synthesis process

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  • Synthesis process of alogliptin benzoate
  • Synthesis process of alogliptin benzoate
  • Synthesis process of alogliptin benzoate

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Embodiment Construction

[0057] In order to enable those skilled in the art to better understand the technical solution of the present invention, the present invention will be described in detail below in conjunction with the accompanying drawings. The description in this part is only exemplary and explanatory, and should not have any limiting effect on the protection scope of the present invention. .

[0058] It should be noted that like numerals and letters denote similar items in the following figures, therefore, once an item is defined in one figure, it does not require further definition and explanation in subsequent figures.

[0059] It should be noted that the orientation or positional relationship indicated by the terms "center", "upper", "lower", "left", "right", "vertical", "horizontal", "inner" and "outer" are Based on the orientation or positional relationship shown in the drawings, or the orientation or positional relationship that the inventive product is usually placed in use, it is onl...

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Abstract

The invention discloses a synthesis process of alogliptin benzoate. The synthesis process comprises the following steps: 1, preparing an initial raw material 6-chlorouracil; 2, preparing 2-((6-chlorine-2, 4-dioxo-3, 4-dihydro-2H-pyrimidine-1-radical)methyl)cyanophenyl; 3, preparing 2-[(6-chlorine-3, 4-dihydro-3-methyl-2, 4-dioxo-1(2H)-pyrimidinyl)methyl]benzonitrile; 4, preparing alogliptin; 5, preparing alogliptin benzoate. According to the invention, the alogliptin benzoate is synthesized by taking cheap and easily available 6-chlorouracil, alpha bromo-o-methylbenzonitrile and (R)-3-aminopiperidine as raw materials through reactions such as alkylation, methylation, affinity substitution, salification and the like; according to the synthetic route, raw materials are cheap and easy to obtain, the synthetic cost is reduced, all steps are classic reactions, and synthesis improvement is easy; the improved process is low in raw material cost, simple to operate, mild in reaction condition,simple in post-treatment and suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of diabetes treatment, in particular to a synthesis process of alogliptin benzoate. Background technique [0002] Diabetes mellitus is a heterogeneous and metabolic chronic lifelong disease characterized by chronic hyperglycemia, which is mainly manifested by chronic hyperglycemia due to insufficient insulin secretion and / or insulin action defects. Clinical syndrome, which can cause atherosclerosis, is also an important risk factor for cardiovascular and cerebrovascular diseases and coronary heart diseases, and can lead to death in severe cases; drug treatment is the main method of diabetes treatment, except for a small number of type II diseases that can be controlled by diet and exercise Except for diabetic patients, they all need to rely on drug treatment. Diabetic drugs are divided into Chinese patent medicine and Western medicine. Western medicine is the main treatment, and Chinese patent medicine is au...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04C07C63/08C07C51/41
CPCC07C51/412C07C63/08C07D401/04
Inventor 张径舟曾祥燕
Owner 重庆化工职业学院
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