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

Method of synthesizing Itraconazole

A synthetic method and the technology of itraconazole are applied in the field of synthesis of itraconazole, which can solve the problems of poor quality and low yield of crude itraconazole, and achieve the goals of increased yield, high yield and reduced cost. Effect

Active Publication Date: 2007-08-08
TIANJIN LISHENG PHARM CO LTD
View PDF0 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 1. The yield of crude itraconazole is low, only about 80%
[0007] 2. Poor quality

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
  • Method of synthesizing Itraconazole
  • Method of synthesizing Itraconazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Add 140 g of water, 45 g of sodium hydroxide, 180 g of toluene, 10 g of hydroxyl, 12 g of methylsulfonate, 0.1 g of hydrazine hydrate, and 1.0 g of TEBA into the reaction flask, and heat up to 110°C for 8 hours under reflux . After the reaction, the temperature was lowered to 40°C, and the lye was separated. Continue to cool down to room temperature, and filter to obtain 17.2 g of crude crystals of itraconazole. The yield is 95.0%, and the impurity content is 0.60%.

Embodiment 2

[0036] Add 140 g of water, 45 g of sodium hydroxide, 180 g of toluene, 10 g of hydroxyl, 12 g of methylsulfonate, 0.2 g of hydrazine hydrate, and 1.0 g of TEBA into the reaction flask, and heat up to 110°C for reflux for 10 hours . According to the operation of Example 1, 16.8 g of crude crystals of itraconazole were obtained, with a yield of 93.0% and an impurity content of 0.80%.

Embodiment 3

[0038] Add 140 g of water, 47 g of potassium hydroxide, 180 g of toluene, 10 g of hydroxyl, 12 g of methylsulfonate, 0.1 g of hydrazine hydrate, and 1.0 g of TEBA into the reaction flask, and heat up to 110°C for reflux reaction 7 Hour. According to the operation of Example 1, 17.1 g of crude crystals of itraconazole were obtained, with a yield of 95.0% and an impurity content of 0.62%.

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 discloses a synthesizing method of yiqukangpyrazole, which comprises the following steps: dissolving sulfonate in the organic solvent; blending with inorganic alkaline solution, antioxidant and quaternary phase-transfering catalyst according to certain rate; adding hydroxy material; heating to 50-110 deg.c; refluxing 5-20 h; cooling to 40deg.c; removing water phase; cooling to 20-30 deg.c; obtaining rough product.

Description

technical field [0001] The invention relates to a synthesis method of itraconazole, which belongs to the technical field of medicine and chemical industry. Background technique [0002] Itraconazole is an azole antifungal drug, which is widely used because of its strong activity, broad antibacterial spectrum and high cure rate. The synthesis process of itraconazole is relatively complicated, including nine steps for the main chain and three steps for the side chain. The last step of its reaction is a condensation reaction, that is, from 2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)-1-piperazinyl]phenyl]-2-(1-methyl Propyl)-]-H-1,2,4-triazol-]-one (referred to as hydroxyl) and cis-[2-(2,4-dichlorophenyl)-2-(1H-1, 2,4-triazole-1-methyl)-1,3-dioxolane-4]-methylsulfonate (referred to as methylsulfonate) is condensed under alkaline conditions to obtain itraconazole Crude. [0003] The process of this condensation reaction is as follows: [0004] [0005] There are following defic...

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
IPC IPC(8): C07D405/14
Inventor 姜根华刘遵利白伟郭辰昱
Owner TIANJIN LISHENG PHARM CO LTD
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com