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Preparation method of acylation derivative of human insulin or analog thereof

A technology for human insulin and analogs, applied in the field of preparation of acylated derivatives, can solve the problems of uneconomical preparation of final products, difficulty in purification, decreased yield and the like

Inactive Publication Date: 2017-03-15
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because in the preparation process of the acylated derivatives of human insulin analogs, insulin analogs occupy most of the cost, and the more steps it participates in the reaction, it may cause a decrease in the yield related to it, resulting in poor preparation of the final product. Economical; this two-step reaction also introduces more impurities, making purification very difficult

Method used

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  • Preparation method of acylation derivative of human insulin or analog thereof
  • Preparation method of acylation derivative of human insulin or analog thereof
  • Preparation method of acylation derivative of human insulin or analog thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Example 1: B28D-N εB29 -(N α -(HOOC(CH 2 ) 14 Preparation of CO)-γ-Glu)-B30E Human Insulin

[0081] 1. Preparation of methylhexadecanedioyl-Glu(OSu)-OMe

[0082] synthetic route:

[0083]

[0084]Take X01 (150g, 524.5mmol), add dry THF (2.5L) at room temperature, then add a catalytic amount of DMF (1.0mL), add oxalyl chloride (49mL) to a 100mL constant pressure dropping funnel, The acid chloride is slowly added dropwise into the reaction flask, during which gas is generated, and the gas needs to be released continuously, and the dropwise addition takes about two hours. After the dropwise addition, stir at room temperature for 1.5 h, then spin dry THF under reduced pressure, add DCM (800 mL) and tert-butanol (500 mL) into the reaction flask, and stir overnight at room temperature. Spin dry tert-butanol and dichloromethane, add dichloromethane (1 L), filter to remove insoluble solids. The filtrate was spin-dried and passed through the column. The required compo...

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Abstract

The invention relates to a preparation method of an acylation derivative of human insulin or analog thereof, and concretely relates to the acylation derivative of the human insulin or the analog thereof, prepared from an acylation group existing in an acid form and the human insulin or the analog thereof through a one-step reaction. The method greatly increases the yield of the final product, omits a purification step, and facilitates industrial production of the acylation derivative of the human insulin or analog thereof.

Description

technical field [0001] The invention relates to a preparation method of acylated derivatives of human insulin or its analogues. Background technique [0002] Diabetes Mellitus (DM) is a common metabolic endocrine disease, which is characterized by chronic hyperglycemia caused by the absolute or relative lack of insulin in the body, or the insensitivity of target tissues to insulin, accompanied by disorders of sugar, fat and protein metabolism. Clinical chronic, systemic metabolic syndrome. It is caused by the interaction of genetic and environmental factors and involves various systems of the human body, including cardiovascular and cerebrovascular, kidney, eye, nerve and other organ complications. It seriously endangers human health and is a lifelong disease. [0003] Diabetes has become a common and frequently-occurring disease. It is the third most life-threatening disease after cancer and cardiovascular and cerebrovascular diseases. According to the statistics of the I...

Claims

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Application Information

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IPC IPC(8): C07K14/62C07K1/06
CPCC07K14/62Y02P20/55
Inventor 王亚里王宏伟刘德玉贾祯鑫宋兴宁张顺吉田伟伟
Owner JIANGSU HENGRUI MEDICINE CO LTD
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