Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of synthetic method of gizzard erosin

A technology for erostin and synthesis method, applied in the direction of organic chemistry and the like, can solve the problems of harsh reaction conditions, unfavorable amplification synthesis, difficulty in separation and purification, etc., and achieves the effects of simple method, better product quality, and good synthesis effect.

Active Publication Date: 2018-04-20
四川威尔检测技术股份有限公司 +2
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The present invention aims to solve the problems of harsh reaction conditions, long synthesis period, very difficult separation and purification, and unfavorable scale-up synthesis in the synthesis method of gizmoerosin in the prior art, and provides a method for synthesizing gizmoerosin, which is simple , fast, and suitable for high-volume synthesis

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of synthetic method of gizzard erosin
  • A kind of synthetic method of gizzard erosin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A kind of synthetic method of gizzard erosin, adopts histamine hydrochloride, acid and oxidant reaction synthesis to obtain 4-hydroxyethylimidazole; 4-hydroxyethylimidazole and chlorination reagent carry out hydroxychlorination reaction, obtain 4-( 2-Chloroethyl) imidazole; 4-(2-Chloroethyl) imidazole, lysine hydrochloride and alkali reaction synthesis to obtain gizzard erosin.

[0037] In the above-mentioned basic technical scheme, acid, oxidant, chlorination reagent and alkali can be selected from conventional reagents in the art to solve the technical problem to be solved by the present invention. In subsequent examples, preferred reagents can achieve better results.

Embodiment 2

[0039] A method for synthesizing gizzard erosin, comprising the following method steps:

[0040] Synthesis of A, 4-hydroxyethylimidazole

[0041] Dissolve histamine hydrochloride in acid and stir to obtain a yellow-green solution. Slowly add an aqueous solution of oxidant at 0°C. After the addition is complete, continue the reaction for 10 h. Evaporate the solvent to obtain a yellow oily liquid. Add a small amount of ethanol and filter the white chlorine. Sodium chloride solid, the filtrate is spin-dried to be the crude product of 4-hydroxyethylimidazole;

[0042] Synthesis of B, 4-(2-chloroethyl) imidazole

[0043] In an ice bath, slowly add a chlorinating reagent to the 4-hydroxyethylimidazole obtained in step A, stir to obtain a yellow solution, react at 0°C for 6 h to obtain a brown clear solution, remove the remaining chlorinating reagent by rotary evaporation to obtain a brown Viscous liquid, add a small amount of water to dissolve, adjust pH to alkaline with sodium ca...

Embodiment 3

[0047] A method for synthesizing gizzard erosin, comprising the following method steps:

[0048] Synthesis of A, 4-hydroxyethylimidazole

[0049] Dissolve histamine hydrochloride in acid and stir to obtain a yellow-green solution. Slowly add an aqueous solution of oxidant at 80°C. After the addition is complete, continue the reaction for 1 hour. Evaporate the solvent to obtain a yellow oily liquid. Add a small amount of ethanol and filter the white chlorine. Sodium chloride solid, the filtrate is spin-dried to be the crude product of 4-hydroxyethylimidazole;

[0050] Synthesis of B, 4-(2-chloroethyl) imidazole

[0051] In an ice bath, slowly add a chlorinating reagent to the 4-hydroxyethylimidazole obtained in step A, stir to obtain a yellow solution, react at 100 °C for 1 h to obtain a brown clear solution, remove the remaining chlorinating reagent by rotary evaporation to obtain a brown Add a small amount of water to dissolve the viscous liquid, adjust the pH to alkaline w...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a synthetic method for gizzerosine and belongs to the technical field of medicines. According to the synthetic method provided by the invention, the steric hindrance of an end amino of lysine is different from that of an alpha-site amino, directly reacts with 4-(2-chloroethyl) imidazole to synthesize a target product through three-step reactions: histamine hydrochloride hydroxylation , chloro reaction and condensation. The method is simple and fast, is suitable for large-scale synthesis, and can be widely applied to related scientific research fields such as toxicology and metabolic experiments.

Description

technical field [0001] The present invention relates to a kind of histamine H 2 A method for synthesizing receptor agonist (S), more specifically, the present invention relates to a method for synthesizing gyostroetin, which belongs to the technical field of medicine. Background technique [0002] Gizzerosine is histamine H 2 Receptor agonists are the main causes of gizzard erosion, loss of appetite, drop in egg laying rate, black spit, death, etc. high. The main cause of the disease is that gizzard erosin can promote a large amount of cAMP production, which in turn leads to a large amount of gastric acid secretion. It is also a drug candidate for the treatment of hyperacidity and osteoporosis. [0003] There are not many literatures on the synthesis of gizmoetin. Andrew Sutherland reported the synthesis of (S)-ginotron by a 10-step harsh reaction, but it needs to be reacted at a low temperature of -78°C and pressurized catalytic hydrogenation of noble metals. The reacti...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/64
CPCC07D233/64
Inventor 赵艳支永刚张凤枰曹俊刘耀敏龙远德
Owner 四川威尔检测技术股份有限公司