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A kind of preparation method of mitiglinide calcium

A technology of mitiglinide calcium and dichloromethane, which is applied in the field of medicine, can solve problems such as being unsuitable for industrial production, and achieve the effects of high industrial production value, high yield, and mild reaction conditions

Inactive Publication Date: 2016-06-15
中国人民解放军联勤保障部队第九六六医院
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Miglinide calcium is an excellent quick-acting hypoglycemic drug. Although there are many synthetic routes reported, most of them are not suitable for industrial production. It is of great significance to find an economical and effective preparation method

Method used

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  • A kind of preparation method of mitiglinide calcium
  • A kind of preparation method of mitiglinide calcium

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Embodiment 1

[0028] Add cis-hexahydroisoquinoline (250.4g, 2mol), anhydrous potassium carbonate (304.0g, 2.2mol), dichloromethane (1000ml) into the reaction flask, keep the temperature at 0-5°C, and stir vigorously, Add a solution of chloroacetyl chloride (271.0g, 2.4mol) in dichloromethane (500ml) dropwise, after the drop, react at room temperature for 2.5h, spot plate monitoring, after the reaction is complete, add 1000ml of water, separate the organic layer, wash with water (1000ml), Wash with saturated brine (1000ml), dry with anhydrous sodium sulfate overnight, distill off dichloromethane under reduced pressure to obtain cis-N-chloroacetylhexahydroisoindole (2) 357.4g oil, yield: 88.6%.

[0029] cis-N-chloroacetylhexahydroisoindole (302.5g, 1.5mol), N-phenylpropionylcamphorsultam (573.0g, 1.65mol), 70% sodium hydride (56.6g, 1.65mol), N,N-Dimethylformamide (900ml) was added into the reaction flask, and stirred vigorously at 50°C for 12h to obtain an alkylated product, which was kept a...

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Abstract

The invention provides a novel preparation method for Mitiglinide calcium hydrate. The method comprises the following steps: adopting cis-hexahydroisoindole as a raw material, conducting acylation reaction, hydrocarbonylation reaction, hydrolysis reaction, and salt forming reaction on the raw material, and obtaining the Mitiglinide calcium hydrate; a one-port process method is adopted for conducting the hydrocarbonylation reaction and the hydrolysis reaction, and the product purity can reach over 99.8%, and the yield can reach over 36%. The preparation method for Mitiglinide calcium hydrate has the advantages of the easy-to-get raw material, mild reaction condition, simple and practicable operation, and relatively high yield, therefore, the method has relatively higher industrial production value, and industrialization has been realized at present.

Description

technical field [0001] The invention relates to the field of medicine, in particular, the invention relates to a preparation method of mitiglinide calcium. Background technique [0002] Bis[(2s)-2-benzyl-3-(cis-hexahydroisoindole-2-carbonyl)propanoic acid] monocalcium dihydrate (mitiglinide calcium), molecular formula C 38 h 48 CaN 2 o 6 2H 2 O, the English name is MitiglinideCalciumHydrate, and the structural formula (I) is as follows: [0003] [0004] Miglinide Calcium was synthesized by Japan Tachibana Pharmaceutical Co., Ltd. and launched in Japan in April 2004. It is used for type Ⅱ diabetic patients whose hyperglycemia cannot be effectively controlled by diet and exercise therapy. Miglinide calcium is the third meglitide drug after repaglinide and nateglinide, which is a derivative of phenylalanine. Miglinide calcium closes the ATP-dependent K channel on the pancreatic β-cell membrane, causing Ca influx, increasing the intracellular Ca concentration and degra...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/44
CPCC07D209/44
Inventor 苑振亭王绍杰
Owner 中国人民解放军联勤保障部队第九六六医院
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