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Method for synthesizing 1-(2-(1-piperidyl) phenyl)-3-methyl butyl amine

A technology of methyl butylamine and methyl butanone, which is used in the synthesis of drugs, drugs for treating diabetes, and the synthesis of 1-[2-phenyl]-3-methylbutylamine, which can solve the problem of high environmental hazards , Inconvenient industrial production, high risk of operation, etc., to achieve the effect of small environmental pollution, mild reaction conditions, and reasonable reaction route

Inactive Publication Date: 2011-05-04
沧州昊瑞医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Most of the oxides used in the above synthesis method are compounds containing heavy metal elements such as chromium and manganese, and these compounds are dangerous to operate and have a high degree of harm to the environment, and usually require special treatment methods, so it is difficult for industrial production cause great inconvenience

Method used

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  • Method for synthesizing 1-(2-(1-piperidyl) phenyl)-3-methyl butyl amine
  • Method for synthesizing 1-(2-(1-piperidyl) phenyl)-3-methyl butyl amine
  • Method for synthesizing 1-(2-(1-piperidyl) phenyl)-3-methyl butyl amine

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preparation example Construction

[0053] In their preparation methods, the remaining contents are consistent.

[0054]

Embodiment 11～15

[0055]Embodiments 11 to 15 are respectively the preparation of 1-[2-(1-piperidinyl)phenyl]-3-methylbutanone

Embodiment 11

[0056] Taking Example 11 as an example, a preparation method of 1-[2-(1-piperidinyl)phenyl]-3-methylbutanone, the reaction scheme is as follows:

[0057]

[0058] The specific operation is as follows: take 5 g of B and mix it with 2.4 g of piperidine, heat to reflux, react for 20 h, TLC detects that the reaction is complete, evaporate the piperidine under normal pressure, add water to the residue, extract with ethyl acetate, combine the organic phases, and dry. Concentration gave oil C, namely 5.9 g of 1-[2-(1-piperidinyl)phenyl]-3-methylbutanone, with a yield of 86.7%.

[0059] Embodiment 12-15 is compared with embodiment 11, and difference is that the parameters involved are different, specifically as shown in the table above: the difference of the amount of substance used; in addition, the amount of substance obtained by each embodiment is also different (not given in the table above). out). In their preparation methods, the remaining contents are consistent.

[0060] ...

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Abstract

The invention discloses a method for synthesizing intermediate (s)1-(2-(1-piperidyl) phenyl)-3-methyl butyl amine of repaglinide used for treating diabetes by a hydrogen peroxide oxidation method, comprising the steps of taking o-fluorobenzaldehyde as a raw material; obtaining alcohol through Grignard reaction; oxidizing the alcohol into ketone under the action of oxidizers of hydrogen peroxide and sodium hypochlorite; and obtaining target product (s)1-(2-(1-piperidyl) phenyl)-phenyl)-3-methyl-butyl amine through a series of reactions. The synthesis method has the characteristics of mild reaction conditions, less environmental pollution and high safety and efficiency, is simple in operation. The invention can be used for synthesis of 1-(2-(1-piperidyl) phenyl)-3-methyl butyl amine, and the synthesized target product is one of intermediates and is further used for preparing repaglinide used for treating diabetes by condensation.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to the synthesis of drugs for the treatment of diabetes, specifically an intermediate of the drug repaglinide for the treatment of diabetes, namely 1-[2-(1-piperidinyl)phenyl]- Synthetic method of 3-methylbutylamine. Background technique [0002] Repaglinide chemical name S(+)-2-ethoxy-4-[N-{1-(2-(1-piperidinyl)phenyl]-3-methyl-1-butane Base}aminocarbonylmethyl]benzoic acid is an oral non-sulfonylurea insulin release accelerator for the treatment of type II diabetes. It is characterized by short duration, good safety, and synergistic effect with biguanide drugs, which can be administered alone or in combination with other hypoglycemic drugs to increase the curative effect. [0003] Repaglinide is formed by condensation of two intermediates, one of which is (S)1-[2-(1-piperidinyl)phenyl]-3-methylbutylamine. The synthesis method of body has been reported, for example: [0004] In the...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/135
Inventor 王浩王建利刘强刘惠娴
Owner 沧州昊瑞医药科技有限公司