Polynuclear compound and preparation method and application thereof

A polynuclear compound and compound technology, applied in the fields of medicinal chemistry and pharmacotherapeutics, can solve the problems of poor molecular stability and unavailability of drug efficacy, and achieve the effect of easy operation, significant hypoglycemic effect, and prolonged metabolism time.

Inactive Publication Date: 2016-06-01
PI & PI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the molecular stability of this compound under heating, acid, alkali and oxidation conditions is poor, so that its medicinal effect cannot be exerted.

Method used

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  • Polynuclear compound and preparation method and application thereof
  • Polynuclear compound and preparation method and application thereof
  • Polynuclear compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] (1a) Synthesis of berberine derivatives: Weigh 1 part by weight of berberine, add 150 (150 to 200) parts by weight of acetonitrile, heat 85 parts to boiling, add X (CH 2 ) n Y40 (20-40) parts by weight, reflux for 3 hours, concentrate the reaction solution to 50 (50-100) parts by weight, cool to obtain crystal A, filter, wash the crystals with an appropriate amount of acetonitrile, combine the washing liquid and the filtrate, Acetonitrile was recovered, the residue was dissolved in 30 parts by weight of methanol, cooled to obtain crystal B, filtered, crystal B was washed with methanol, and crystal A and crystal B were combined to obtain a berbererythrine derivative with a calculated yield of 56.34%. Among them, the X(CH of the present embodiment 2 ) n In Y, both X and Y are Br, n=2, and the obtained berberine derivative is berberine-9-oxyethyl bromide. In other embodiments, X and Y can be independently O, S, F, Cl or I, and n can be an integer such as 1, 3, 4, etc.≦3...

Embodiment 2

[0086] X(CH of this embodiment 2 ) n In Y, both X and Y are Cl, and n=3. According to the preparation method of Example 1, the compound with the structure shown in formula (I) was prepared.

Embodiment 3

[0088] X(CH of this embodiment 2 ) n In Y, both X and Y are S, n=4, and the compound with the structure shown in formula (I) is prepared according to the preparation method of Example 1.

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PUM

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Abstract

The invention discloses a polynuclear compound which is of the structure as indicated in the general formula (1).The invention further discloses a preparation method of the polynuclear compound and application of the polynuclear compound to preparation of medicine for treating diabetes.According to the methylated polynuclear compound, under the condition that medicine effects are maintained unchanged, stability of the polynuclear compound is improved.

Description

technical field [0001] The present invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to a methylated multinuclear molecular compound, a preparation method of the compound and an application in the preparation of medicines for treating diabetes. Background technique [0002] Diabetes is a huge and growing global problem with an increasing burden on society; in all countries, those in the lower classes of society are more likely to develop diabetes and bear a relatively heavier burden. Diabetes is not just a simple health problem. Solving the problem of diabetes requires specific policies and actions from multiple aspects of society. [0003] Commonly used diabetes treatment drugs in clinical practice include: [0004] (1) Insulin and its analogs [0005] Insulin preparations have gone through the stages of animal-derived insulin and genetically engineered human insulin. The development of insulin analogues and their use methods a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03A61K31/4375A61P3/06A61P3/10
CPCC07D455/03
Inventor 袁晓周东斌范建军张伟
Owner PI & PI BIOTECH
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