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A kind of hypoglycemic drug and preparation method thereof

A drug and hypoglycemic technology, which is applied in the field of preparation of the hypoglycemic drug, can solve the problems of metallic odor and weak efficacy of metformin, and achieve the effects of low effective dose, significant hypoglycemic effect, and strong alkalinity reduction

Active Publication Date: 2017-05-31
青岛嘉源汇美生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug effect of metformin is relatively weak, and it is often necessary to take a large dose of 1g / day to increase the curative effect. Biguanide is the strongest organic base. After high-concentration metformin is taken, the high-concentration metformin adheres to the digestive tract mucosa and causes irritation. Nausea, vomiting, loss of appetite, metallic taste in the mouth, diarrhea, etc.

Method used

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  • A kind of hypoglycemic drug and preparation method thereof
  • A kind of hypoglycemic drug and preparation method thereof
  • A kind of hypoglycemic drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 SI-0220 (A is sitagliptin)

[0035]

[0036] Take 12.01g (0.1mol) of tartronic acid and 38.01g (0.15mol) of Woodward's reagent K, add 1L of anhydrous acetonitrile, cool to 0°C under stirring, add 13.36g (0.1mol) of triethylamine, °C and stirred for 1 hour. Separately take 40.82g (0.1mol) of sitagliptin free base and 12.95g (0.1mol) of metformin free base, dissolve in 1L of anhydrous acetonitrile and 200mL of DMF, add 13.36g (0.1mol) of triethylamine, mix well, Slowly drop into the above reaction solution at 0°C, stir at room temperature for 72 hours after the dropwise addition, and monitor the reaction by HPLC. After the reaction is completed, evaporate to dryness under reduced pressure, add 200mL of water, stir for 30 minutes, filter with suction, and filter the cake with ethanol -Water (4:1) recrystallization, that is.

[0037] Preparation of free base: get sitagliptin or metformin 100g, add 500ml water and 1000ml dichloromethane, slowly add 500ml of 4M...

Embodiment 2

[0039] Example 2 SI-0221 (A is vildagliptin)

[0040]

[0041] Using vildagliptin instead of sitagliptin was prepared in a similar manner to Example 1 to obtain the target compound. Mass spectrum (+ESI, m / z): 517.58[M+H] + .

Embodiment 3

[0042] Example 3 SI-0222 (A is alogliptin)

[0043]

[0044]Using alogliptin instead of sitagliptin, it was prepared in a similar manner to Example 1 to obtain the target compound. Mass Spectrum (+ESI, m / z): 686.74[M+H] + .

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Abstract

The invention relates to a novel hypoglycemic agent. In addition, the invention further relates to a drug mixture which takes the hypoglycemic agent as an effective medical component, and optimally contains one or more excipients or carriers, or a drug composition used for treating diabetes combined with besity. Moreover, the invention further relates to a preparation method of the hypoglycemic agent.

Description

technical field [0001] The present invention relates to hypoglycemic drugs, especially A-Z-B type derivatives, more particularly peptide bond derivatives of amino-containing hypoglycemic drugs (A)-propanol diacid (Z)-metformin (B), the derivatives and The salt can be used as a hypoglycemic agent for treating diabetes; the invention also relates to a preparation method of the hypoglycemic drug. Background technique [0002] Diabetes is a group of metabolic diseases characterized by hyperglycemia. Hyperglycemia is caused by defective insulin secretion or impaired biological action, or both. The long-term high blood sugar in diabetes leads to chronic damage and dysfunction of various tissues, especially the eyes, kidneys, heart, blood vessels, and nerves. It is estimated that the prevalence of diabetes among adults over the age of 20 in my country is 9.7%. The total number of adults with diabetes in China is 92.4 million, including 43.1 million in rural areas and 49.3 million...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04C07D207/16C07D473/04C07D401/04C07C279/26C07C277/08A61K31/4985A61K31/40A61K31/522A61K31/513A61K31/155A61K31/16A61P3/10A61P3/04
CPCC07C277/08C07C279/26C07C2601/14C07D207/16C07D473/04C07D487/04
Inventor 管文珍李小琳王晓明
Owner 青岛嘉源汇美生物科技有限公司
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