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Valganciclovir hydrochloride preparation method

A technology of valganciclovir hydrochloride and hydrochloric acid, applied in the field of valganciclovir hydrochloride preparation, can solve the problems of inability to meet industrial production requirements, inability to continuous production, long reaction time, etc., and achieves a high degree of automation, material in and out Convenience and controllable reaction temperature

Inactive Publication Date: 2021-02-26
沃德药业(安徽)股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the main production process adopts batch-type hydrogenation reactor, and the monoester is deprotected under the catalytic hydrogenation of palladium carbon. The reaction time is too long, and continuous production cannot be performed, which cannot meet the requirements of industrial production.

Method used

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  • Valganciclovir hydrochloride preparation method
  • Valganciclovir hydrochloride preparation method
  • Valganciclovir hydrochloride preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] like figure 1 The shown equipment for preparing valganciclovir hydrochloride includes material tank 3, tubular reactor 4, hydrogen tank 5, receiving tank 6 and reactor (not shown in the figure), and material tank 3 and tube The first pump body 1 is arranged between the reactors 4, and the second pump body 2 is arranged on the tubular reactor 4. The inlet and outlet of the tubular reactor 4 adopt 316 steel high-quality check valves, which are stable and safe.

[0033] use as figure 1 Shown equipment prepares a kind of valganciclovir hydrochloride, comprises the steps:

[0034] S1, loading catalyst: before loading the catalyst, the tubular reactor 4 is checked, and the reactor is required to be unimpeded, clean, free of debris, and replaced with nitrogen gas (purging and drying with nitrogen gas), and then 15kg 5% Pd / C is filled in tubular reactor 4 (tubular reactor 4 adopts conventional horizontal tubular reactor, model JHF-1, Nantong Walchi Petrochemical Engineering ...

Embodiment 2

[0045] use as figure 1 Shown equipment prepares a kind of valganciclovir hydrochloride, comprises the steps:

[0046] S1, loading catalyst: before loading the catalyst, the tubular reactor 4 is checked, and the reactor is required to be unimpeded, clean, free of debris, and replaced with nitrogen gas (purging and drying with nitrogen gas), and then 205kg 5% Pd / C is filled in tubular reactor 4 (tubular reactor 4 adopts conventional horizontal tubular reactor, model JHF-1, Nantong Walchi Petrochemical Engineering Co., Ltd.);

[0047] S2, reactant dissolving: put 120kg monoester and 120kg methanol, 20kg concentrated hydrochloric acid into the 500L reactor and stir to dissolve, and put the dissolved material into the material tank 3;

[0048] S3, open the first pump body 1 to pass the material in the material tank 3 into the tubular reactor 4, and then open the second pump body 2, so that the material circulates in the tubular reactor 4;

[0049] S4. Detect the content of oxyge...

Embodiment 3

[0056] based on figure 1 As shown in the equipment for preparing valganciclovir hydrochloride, the receiving tank 6 is communicated with the material tank 3 through a pipeline, and the pipeline is provided with a valve (this pipeline and valve are not shown in the figure).

[0057] Utilize above-mentioned equipment to prepare a kind of valganciclovir hydrochloride, comprise the steps:

[0058] S1, loading catalyst: before loading the catalyst, the tubular reactor 4 is checked, and the inside of the reactor is required to be unimpeded, clean, free of debris, and qualified for replacement with nitrogen (purging and drying with nitrogen), and then 210kg 5% Pd / C is filled in tubular reactor 4 (tubular reactor 4 adopts conventional horizontal tubular reactor, model JHF-1, Nantong Walchi Petrochemical Engineering Co., Ltd.);

[0059] S2, reactant dissolution: put 120kg monoester and 120kg methanol, 24kg concentrated hydrochloric acid into 500L reactor and stir to dissolve;

[006...

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Abstract

The invention discloses a valganciclovir hydrochloride preparation method, and belongs to the technical field of drug preparation. The preparation method comprises the steps: mixing a monoester substance, methanol and hydrochloric acid, dissolving, introducing into a material tank, introducing the dissolved substance in the material tank into a tubular reactor pre-filled with a catalyst through apump body, and enabling the material to circularly move in the tubular reactor through the other pump body, starting the circular reaction after compressed hydrogen is introduced, introducing nitrogeninto the tubular reactor after the reaction is finished, discharging the material into the receiving tank from the tubular reactor, and then impurity removal, decoloration and crystallization treatment is performed on the material to obtain a finished product. The tubular reactor is used as a main reaction place so that the reaction time can be greatly shortened, and the conversion efficiency isimproved; the catalyst filling in the reactor is easy to recover so that the cost can be saved; the automation degree is high, and the industrial continuous production requirement is met.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a preparation method of valganciclovir hydrochloride. Background technique [0002] Valganciclovir is a synthetic 2-deoxyguanosine analog, which is the prodrug of the antiviral drug ganciclovir (ganciclovir), which can greatly reduce the toxicity of ganciclovir. At present, the main production process adopts a batch hydrogenation reactor, and the monoester is deprotected under palladium-carbon catalytic hydrogenation. The reaction time is too long, and continuous production cannot be performed, which cannot meet the requirements of industrial production. [0003] The tubular reactor has small backmixing, so the volumetric efficiency (production capacity per unit volume) is high, and it is especially suitable for occasions that require a high conversion rate or have side reactions in series. In addition, the tubular reactor can realize segmental temperature control. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18
CPCC07D473/18
Inventor 何亚奇钟俊生
Owner 沃德药业(安徽)股份有限公司
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