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A kind of diflavin, its preparation method and application

A technology of biflavin and baicalein, applied in the field of medicinal chemistry and pharmacotherapeutics, to achieve the effect of improving absorption, facilitating large-scale industrial production, and enhancing drug efficacy

Active Publication Date: 2017-10-24
PI & PI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are no public or related reports on the patents and related research on the chemical synthesis of berberine and baicalein into new multi-nuclear molecules

Method used

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  • A kind of diflavin, its preparation method and application
  • A kind of diflavin, its preparation method and application
  • A kind of diflavin, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] (1a) Synthesis of berberine derivatives: Weigh 1 part by weight of berberine, add 150 (150-200) parts by weight of acetonitrile, heat to boiling at 85°C, add X(CH 2 ) n Y 40 (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 crystal A with an appropriate amount of acetonitrile, washing liquid and filtrate Combine and recover acetonitrile. The filter residue was dissolved with 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, X(CH in this embodiment 2 ) n Y, X, and Y are all Br, n=4, and the gained berberine derivative is berberine-9-oxobutyl bromide, and its 1 H NMR picture as figure 1 as shown, 13 C NMR picture as figure 2 shown. in, figure 1 The attribution of H in is shown in Ta...

Embodiment 2

[0091] In addition to the amount of acetonitrile, X(CH 2 ) n Except that the amount of Y and the concentration of the reaction solution are different, the preparation method of the diflavin in this implementation is basically the same as that of Example 1. Among them, the X(CH of the present embodiment 2 ) n Y, X, Y are all Cl, n=5.

Embodiment 3

[0093] In addition to the amount of acetonitrile, X(CH 2 ) n Except that the amount of Y and the concentration of the reaction solution are different, the preparation method of the diflavin in this implementation is basically the same as that of Example 1. Among them, the X(CH of the present embodiment 2 ) n Y, X and Y are all S, n=6.

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Abstract

The invention discloses a berberrubine and baicalein compound with the structure shown in the general formula (I). The invention further discloses a preparing method of the compound, and the compound is formed by synthesizing berberrubine and baicalein. The invention furthermore discloses application of the compound to preparation of a drug for treating ulcerative enteritis. Compared with berberrubine and baicalein, toxicity of the polynuclear molecular compound is reduced substantially, absorption is improved substantially, bioavailability is improved, the metabolism time is prolonged, the long-acting effect can be achieved, and the pharmacological effects of resisting ulcerative enteritis and pathogenic bacteria are enhanced.

Description

technical field [0001] The invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to a diflavin, a preparation method of the compound and an application in the preparation of medicines for treating ulcerative enteritis. Background technique [0002] Ulcerative colitis (UC), also known as chronic nonspecific ulcerative colitis or idiopathic ulcerative colitis, is a common chronic intestinal disease and a multifactorial and multilayered disease with unknown causes. nonspecific inflammation. The lesions are mainly in the mucosa and submucosa of the colon, showing continuous and diffuse distribution, most of which involve the rectum and sigmoid colon. The main clinical manifestations are abdominal pain, diarrhea, mucus pus and blood in the stool, tenesmus, etc. Some patients have extraintestinal manifestations, such as joint, liver and bile duct diseases, and eye and skin damage; Between 20 and 50 years old, but no significant sex differ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61K31/4375A61P1/04A61P1/00
CPCC07D455/03
Inventor 李卫民袁晓荣向路周东斌
Owner PI & PI BIOTECH
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