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Poly-nuclear molecular compound and preparation method and application thereof

A technology of multinuclear molecules and compounds, applied in the fields of medicinal chemistry and pharmacotherapeutics

Active Publication Date: 2015-01-21
PI & PI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0057] At present, there are no public or related reports on the patents and related research on the chemical synthesis of berberine and magnolol into new multinuclear molecules

Method used

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  • Poly-nuclear molecular compound and preparation method and application thereof
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  • Poly-nuclear molecular compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0124] An embodiment of the multinuclear molecular compound of the present invention, the multinuclear molecular compound described in this embodiment is prepared by the following method:

[0125] (1a) Synthesis of berberine derivatives: Weigh 1 part by weight of berberine, add 150 parts by weight of acetonitrile, heat to boiling at 85°C, add X(CH 2 ) n Y40 parts by weight, reflux for 3 hours, concentrate the reaction solution to 50 parts, cool and crystallize, filter, wash the crystals with an appropriate amount of acetonitrile, combine the washing liquid with the filtrate, recover acetonitrile, dissolve the residue with 30 parts by weight of methanol, cool and crystallize, filter, Wash the crystals with methanol, and merge with the above-mentioned crystals to obtain a sample yield of 56.34%, a berberine derivative with a purity of more than 95%, wherein the X(CH 2 ) n In Y, both X and Y are Br, n=2, and the obtained berberine derivative is berberine-9-oxyethyl bromide, w...

Embodiment 2

[0147] An embodiment of the multinuclear molecular compound of the present invention, the multinuclear molecular compound described in this embodiment is prepared by the following method:

[0148] (1a) Synthesis of berberine derivatives: weigh 1 part by weight of berberine, add 200 parts by weight of acetonitrile, heat to boiling at 85°C, add X(CH 2 ) n 20 parts by weight of Y, reflux for 3 hours, concentrate the reaction solution to 100 parts, cool and crystallize, filter, wash the crystals with an appropriate amount of acetonitrile, combine the washing liquid with the filtrate, recover acetonitrile, dissolve the residue with 30 parts by weight of methanol, cool and crystallize, filter, Wash the crystals with methanol, and merge with the above-mentioned crystals to obtain a sample yield of 56.34%, a berberine derivative with a purity of more than 95%, wherein the X(CH 2 ) n In Y, both X and Y are Cl, n=3;

[0149](2a) Mix 1.2 parts by weight of the berberine derivative o...

Embodiment 3

[0152] An embodiment of the multinuclear molecular compound of the present invention, the multinuclear molecular compound described in this embodiment is prepared by the following method:

[0153] (1a) Synthesis of berberine derivatives: Weigh 1 part by weight of berberine, add 160 parts by weight of acetonitrile, heat to boiling at 85°C, add X(CH 2 ) n Y30 parts by weight, reflux for 3 hours, concentrate the reaction solution to 80 parts, cool and crystallize, filter, wash the crystals with an appropriate amount of acetonitrile, combine the washing liquid with the filtrate, recover acetonitrile, dissolve the residue with 30 parts by weight of methanol, cool and crystallize, filter, Wash the crystals with methanol, and merge with the above-mentioned crystals to obtain a sample yield of 56.34%, a berberine derivative with a purity of more than 95%, wherein the X(CH 2 ) n In Y, both X and Y are S, n=4;

[0154] (2a) Mix 1.2 parts by weight of the berberine derivative obtain...

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Abstract

The invention discloses a poly-nuclear molecular compound. The poly-nuclear molecular compound is prepared by synthesizing berberrubine and magn olol. A brand new poly-nuclear molecular compound is provided for the first time. The poly-nuclear molecular compound is prepared by synthesizing berberrubine and magnolol, and the medicament metabolism loops of absorption, distribution, metabolism and excretion of a single component or a mixture of two components are changed. Compared with berberrubine and magnolol, the obtained poly-nuclear molecular compound has the advantages of remarkably lowered toxicity being only 10 percent that of berberrubine and magnolol, remarkable increase in absorption rate, higher bioavailability, longer metabolism time, long-acting effect and enhanced blood sugar reducing effect. Moreover, the invention further discloses a preparation method of the poly-nuclear molecular compound, and application of the compound to preparation of diabetes drugs.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and pharmacotherapeutics, and specifically relates to a multi-nuclear molecular compound synthesized from berberine and magnolol, a preparation method thereof and an application in preparing medicine for treating diabetes. Background technique [0002] Diabetes is a chronic disease that occurs when the pancreas does not produce enough insulin or the body cannot effectively use the insulin it produces. Insulin is a hormone that regulates blood sugar. Hyperglycemia, or elevated blood sugar, is a common result of uncontrolled diabetes and over time can cause serious damage to many systems in the body, especially the nerves and blood vessels. Diabetes is generally divided into type 1 diabetes, type 2 diabetes and gestational diabetes. [0003] Impaired Glucose Tolerance (IGT) and Impaired Fasting Glucose (IFG) refer to an intermediate state in the transition stage between normal and diabetic blood...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61P3/10
CPCC07D455/03A61P3/10C07D491/147
Inventor 李卫民袁晓荣向路周东斌
Owner PI & PI BIOTECH
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