Method for producing itraconazole bulk drug

A technology of itraconazole and raw materials, applied in the field of production of itraconazole raw materials, can solve the problems of cumbersome procedures, long operation time, high energy consumption, etc., and achieve the reduction of the number of operators, the improvement of product yield, and the production The effect of labor intensity reduction

Active Publication Date: 2020-01-31
SINOPEC SHANGHAI ENG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention is the problem of high energy consumption, long operation time and cumbersome procedures in the prior art, and a new method for producing itraconazole bulk drug is provided

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] This method is implemented in the raw material drug workshop of a certain pharmaceutical factory, with an annual output of 2 tons of itraconazole.

[0021] The production process of itraconazole bulk drug includes the preparation of nitro, amine, ring-closing, alkyl, hydroxyl, triazole and mesylate.

[0022] The preparation of itraconazole mainly includes two parts of main chain and side chain. The main chain is prepared as follows: the nitro compound is used as a starting material, and the fine nitro compound is obtained by dissolving with dioxane, crystallizing, filtering and drying. Under the catalysis of palladium carbon catalyst, in THF solvent, the nitro group in the nitro compound is reduced by hydrogen to carry out hydrogenation reaction, and then the amine compound is obtained through filtration, distillation, drying, etc. Under the catalysis of p-toluenesulfonic acid and sodium methoxide, in anhydrous ethanol solvent, amines react with methyl carbazate and tr...

Embodiment 2

[0035] According to the conditions and steps described in Example 1, the reaction temperature control system of the present invention is applied to the nitro substance preparation section, and the heat exchange medium is a mixture of 40% ethylene glycol and water. The three step temperatures of the same heat exchange medium are 160°C, 30°C, and -10°C.

[0036] Got the following data:

[0037] Product yield of itraconazole: 95%;

[0038] Public works consumption: the electricity used is equivalent to the production cost of 11,000 yuan / ton;

[0039]Reactor life: Slight abrasion begins to appear after 4-5 years of normal operation;

[0040] Section operator setting: intermittent operation, the number of operators on duty is 1;

[0041] Batch production auxiliary time: 10min.

Embodiment 3

[0043] According to the conditions and steps described in Example 1, the reaction temperature control system of the present invention is applied to the ring-closing compound preparation section, and the heat exchange medium is a mixture of 40% ethylene glycol and water. The three step temperatures of the same heat exchange medium are 130°C, 100°C, and -40°C.

[0044] Got the following data:

[0045] Product yield of itraconazole: 96%;

[0046] Public works consumption: the electricity used is equivalent to the production cost of 15,000 yuan / ton;

[0047] Reactor life: Slight abrasion begins to appear after 4-5 years of normal operation;

[0048] Section operator setting: intermittent operation, the number of operators on duty is 1;

[0049] Batch production auxiliary time: 10min.

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Abstract

The invention relates to a method for producing an itraconazole bulk drug and mainly aims to solve the problems of high energy consumption, long operation time and tedious procedure in the prior art. According to the method for producing the itraconazole bulk drug, temperature change of liquids in reactors is controlled in accordance with high, medium and low temperatures of the same heat exchange medium, and adding quantities of toxic materials are controlled by means of concentration in the reactors as well as linkage arrangement of pressure sensors and toxic material pipe flow control valves; rotating speeds of stirring shafts are controlled by means of linkage arrangement of liquid level sensors and variable-frequency motors in the reactors; the medium is controlled to heat and cool reaction liquids by means of linkage arrangement of temperature sensors in the reactors and reactor jacket medium pipeline switch valves. The problems are solved better with the technical scheme, and the method can be used for producing the itraconazole bulk drug.

Description

technical field [0001] The invention relates to a method for producing itraconazole bulk drug. Background technique [0002] The production process of itraconazole bulk drug includes: preparation of nitro compounds, preparation of amine compounds, preparation of cyclic compounds, preparation of alkyl compounds, preparation of hydroxyl compounds, preparation of triazole compounds, preparation of mesylate and other processes. Many reactions in the above process require high temperature control of the reaction solution. The cooling and heating of the reaction liquid can be realized through the alternating action of cold and hot media on the jacket (or coil) of the reactor. Generally, saturated steam is used as the heat medium, cooling water or low-temperature brine is used as the refrigerant, and a circulating water pipeline is used separately for buffering the cooling process and cooling of the reaction liquid in a special environment in winter, and a compressed air pipeline ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/14
CPCC07D405/14Y02P20/10
Inventor 陈琦杨军高志刚丁伟军
Owner SINOPEC SHANGHAI ENG
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