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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
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  • 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

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  • 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%.

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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

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Application Information

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IPC IPC(8): C07D405/14
Inventor 姜根华刘遵利白伟郭辰昱
Owner TIANJIN LISHENG PHARM CO LTD
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