Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Compound having allyl and propanohydrazide pyrimidine structure at terminal, preparation method and application of compound

A compound, pyrimidine technology, applied in the field of medicine, can solve problems such as limited application

Inactive Publication Date: 2018-05-04
FOSHAN SAIWEISI MEDICINE SCI & TECH
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although clozapine, Zyprexa, Vistron, and other antipsychotics have been used to treat both positive and negative (controversial) symptoms of schizophrenia and bipolar disorder, these drugs have not been free from side effects such as Cytopenia, sedation, weight gain, hyperlipidemia and hyperglycemia, all of which limit their use

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
  • Compound having allyl and propanohydrazide pyrimidine structure at terminal, preparation method and application of compound
  • Compound having allyl and propanohydrazide pyrimidine structure at terminal, preparation method and application of compound
  • Compound having allyl and propanohydrazide pyrimidine structure at terminal, preparation method and application of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The synthesis of embodiment 1 compound I-1

[0021]

[0022] Step 1. Synthesis of Compound VI-1

[0023] Compound II (1.32g, 20mmol) was dissolved in 20mL DMSO, stirred at room temperature, KOH solid (2.24g, 40mmol) was added, and stirred at room temperature for 1 hour. Further MeI (III-1, 2.84 g, 20 mmol) was added, and stirring was continued overnight at room temperature. Then tert-butyl acrylate V-1 (2.56 g, 20 mmol) was added, and the stirring was continued for 12 hours, and TLC detection found that the reaction was complete.

[0024] The reaction mixture was carefully poured into 200mL ice water, stirred, and washed with 50mL×3CH 2 Cl 2 After extraction, the extract phases were combined, washed with 100 mL of 5% brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the residue was purified by silica gel column chromatography to obtain compound VI-I,...

Embodiment 2

[0031] The synthesis of embodiment 2 compound 1-2

[0032]

[0033] Step 1. Synthesis of compound VI-2

[0034]Compound II (1.32g, 20mmol) was dissolved in 20mL DMSO, stirred at room temperature, KOH solid (2.24g, 40mmol) was added, and stirred at room temperature for 1 hour. Another 20 mmol of compound III-2 was added, and stirring was continued overnight at room temperature. Then 20 mmol of compound V-2 was added, and the stirring was continued for 12 hours, and TLC detection found that the reaction was complete. The reaction mixture was carefully poured into 200mL ice water, stirred, and washed with 50mL×3CH 2 Cl 2 After extraction, the extract phases were combined, washed with 100 mL of 5% brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the residue was purified by silica gel column chromatography to obtain compound VI-2. ESI-MS, m / z=249 ([M+H] + )....

Embodiment 3

[0039] The synthesis of embodiment 3 compound 1-3

[0040]

[0041] Step 1. Synthesis of compound VI-3

[0042] Compound II (1.32g, 20mmol) was dissolved in 20mL DMSO, stirred at room temperature, KOH solid (2.24g, 40mmol) was added, and stirred at room temperature for 1 hour. Another 20 mmol of compound III-2 was added, and stirring was continued overnight at room temperature. Then 20 mmol of compound V-3 was added, and the stirring was continued for 12 hours, and TLC detection found that the reaction was complete. The reaction mixture was carefully poured into 200mL ice water, stirred, and washed with 50mL×3CH 2 Cl 2 After extraction, the extract phases were combined, washed with 100 mL of 5% brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the residue was purified by silica gel column chromatography to obtain compound VI-3. ESI-MS, m / z=263 ([M+H] + )...

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 belongs to the technical field of medicines, and particularly relates to a compound having an allyl and propanohydrazide pyrimidine structure at a terminal, a preparation method and application of the compound. The formula (1) is shown in the description, wherein R is selected from H and alkyl of C1-C5.

Description

technical field [0001] The invention belongs to the technical field of medicine. Specifically, the present invention relates to a class of compounds containing an allyl propionohydrazide structure at the end, a preparation method thereof, and an application thereof in the preparation of drugs for treating mental diseases. Background technique [0002] Symptoms of schizophrenia are generally divided into three categories: positive, negative and cognitive. Positive symptoms include hallucinations, delusions, and disorganized behavior, while negative symptoms are characterized by a lack of pleasure and / or interest in life. Cognitive deficits include difficulty organizing thoughts and prioritizing tasks. Patients with bipolar disorder typically display cyclical mood swings (with or without psychotic features) from severe depression to severe mania. Schizophrenia and bipolar disorder are among the most severe types of mental disorders causing overlapping cognitive deficits and...

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 Applications(China)
IPC IPC(8): C07D239/42A61P25/18
CPCC07D239/42
Inventor 蔡子洋
Owner FOSHAN SAIWEISI MEDICINE SCI & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com