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2,4,5-triamido-6-hydroxy pyrimidine formate, preparation method and application

A hydroxypyrimidine and triamino technology, which is applied in the fields of 2,4,5-triamino-6-hydroxypyrimidine formate, preparation and application, can solve the problems of high salt, unfriendly environment, etc. The effect of short production route and reduced content

Active Publication Date: 2018-01-19
潍坊奥通药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a result, a large amount of high-salt and heavy-acid wastewater is produced, which is seriously unfriendly to the environment

Method used

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  • 2,4,5-triamido-6-hydroxy pyrimidine formate, preparation method and application
  • 2,4,5-triamido-6-hydroxy pyrimidine formate, preparation method and application
  • 2,4,5-triamido-6-hydroxy pyrimidine formate, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Mix 155g of 2,4-diamino-5-nitroso-6-hydroxypyrimidine (hereinafter referred to as "nitroso", MW155.11, 1.00mol) with 1800mL drinking water, make a certificate, and pump 3L Hydrogenation kettle. Turn on the hydrogenation tank and stir, and inhale 160g of 30% lye (sodium hydroxide aqueous solution, 1.2mol) and 18g of W-type Raney nickel.

[0057] After feeding, fill the air with high-purity nitrogen and replace it 3 times; then replace it with hydrogen 3 times.

[0058] After the replacement, pressurize with hydrogen to 0.5-0.6MPa, heat and raise the temperature to 50-60°C. Keeping warm, keeping the pressure, and stirring rapidly until the hydrogen is no longer absorbed (that is, the hydrogen pressure in the kettle does not drop within 30 minutes).

[0059] In advance, 380 g (MW46.03, 4.13 mol) of formic acid solution with a mass percent concentration of 50% was added into a 3L three-necked flask, replaced with nitrogen for 3 times, stirred and protected by nitrogen, an...

Embodiment 2

[0068] Mix 155g of 2,4-diamino-5-nitroso-6-hydroxypyrimidine (hereinafter referred to as "nitroso", MW155.11, 1.00mol) with 1500mL of drinking water, make a slurry, and pump it into 3L hydrogenation kettle. Open the hydrogenation tank and stir, inhale 200g of 30% lye (1.5mol) and 18g of W-type Raney nickel.

[0069] After feeding, fill the air with high-purity nitrogen and replace it 3 times; then replace it with hydrogen 3 times.

[0070] After the replacement, pressurize with hydrogen to 0.6-0.8MPa, heat and raise the temperature to 50-60°C. Heat preservation, pressure maintenance, and rapid stirring until no hydrogen is absorbed.

[0071] In advance, 300 g (MW46.03, 3.26 mol) of 50% formic acid was added into a 3L three-necked flask, replaced with nitrogen for 3 times, stirred, and kept under nitrogen protection for use.

[0072] After the hydrogenation reaction, the excess hydrogen in the kettle was drained, and then replaced with high-purity nitrogen for 3 times; then ...

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Abstract

The invention discloses 2,4,5-triamido-6-hydroxy pyrimidine formate and a preparation method. The preparation method comprises the following steps: enabling 2,4-diamido-5-nitro-6-hydroxy pyrimidine toreact with hydrogen in catalyst A and alkaline solution B, and obtaining 2,4,5-triamido-6-hydroxyl pyrimidine; and enabling a hydrogenation product to perform the salt forming reaction with formic acid to obtain 2,4,5-triamido-6-hydroxy pyrimidine formate. The invention discloses a method for preparing guanine by utilizing the 2,4,5-triamido-6-hydroxy pyrimidine formate. The preparation method isshort in production route, and high in molar yield, wherein the total molar yield is 90 percent or higher. The solvent can be recycled and generally used, the content of the salt and strong acid in the production wastewater can be greatly reduced, and the emission amount is little. The pyrimidine formate is a brand new compound. The pyrimidine formate is used for substituting the pyrimidine sulfate to prepare the guanine, so that a great amount of sulfate can be prevented from flowing into the production wastewater.

Description

technical field [0001] The invention belongs to the fields of preparation technology and application of key intermediates of Lowe antiviral drugs, and specifically relates to a 2,4,5-triamino-6-hydroxypyrimidine formate, a preparation method and an application. Background technique [0002] Clovir drugs, mainly including acyclovir, ganciclovir, valacyclovir and faciclovir, are broad-spectrum antiviral drugs. It is clinically used to treat herpes simplex and diseases related to HSV infection, such as erythema multiforme, herpes zoster, first and recurrent genital herpes, HSV encephalitis, chickenpox, herpes zoster and VZV encephalitis, AIDS, Pneumonia, enteritis and retinitis caused by severe CMV infection in organ transplantation and malignant tumor patients. [0003] Guanine is a key intermediate for the preparation of acyclovir (ACV), ganciclovir (GCV), valacyclovir (FCV) and the like. Its chemical name is: 2-aminopurine, and its molecular formula is: C 5 h 5 N 5 O, t...

Claims

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Application Information

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IPC IPC(8): C07D239/50C07D473/18C07C51/41C07C53/06
Inventor 杨栽根魏海鹏晏金华刘晓磊
Owner 潍坊奥通药业有限公司
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