2-amino-6-chloropurine as well as synthesis method, intermediate and application thereof

A synthetic method, the technology of chloropurine, which is applied in the field of medicine, can solve the problems of high equipment requirements, viscous materials, difficulty in suction filtration/centrifugation, etc., and achieve the effect of cheap and easy-to-obtain raw materials, few reaction steps, and good industrial prospects

Active Publication Date: 2019-12-31
NANJING REDWOOD FINE CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with the previous synthesis processes, this synthesis process is relatively reasonable, but this process will produce a large amount of three wastes, and the post-treatment is also relatively cumbersome, and the material is viscous, and suction filtration / centrifugation is very difficult, requiring high equipment.

Method used

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  • 2-amino-6-chloropurine as well as synthesis method, intermediate and application thereof
  • 2-amino-6-chloropurine as well as synthesis method, intermediate and application thereof
  • 2-amino-6-chloropurine as well as synthesis method, intermediate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Such as figure 1 As shown, the present embodiment 1 provides a kind of synthetic method of 2-amino-6-chloropurine, comprises the following steps: step S1, one reaction, i.e. ethyl cyanoacetate, chloroformamidine hydrochloride, liquid ammonia and Sodium mixed reaction to generate intermediate; step S2, secondary reaction, that is, intermediate and formic acid mixed reaction; step S3, after cooling, slowly add 10% sodium hydroxide solution to the product of the secondary reaction, and thoroughly Mix until the mixture is just alkaline with litmus; and step S4, filter with a Buchner funnel, collect the solid by suction, and then dry to obtain the 2-amino-6-chloropurine.

[0033] Optionally, the molar ratio of ethyl cyanoacetate, chloroformamidine hydrochloride, liquid ammonia, sodium, and formic acid is 1:1.1-1.2:2-3:0.1:1-1.5.

[0034] The synthesis method of the present embodiment 1 selects ethyl cyanoacetate, chloroformamidine hydrochloride, and liquid ammonia as raw ma...

Embodiment 2

[0047] On the basis of Example 1, this Example 2 provides a kind of 2-amino-6-chloropurine, its structural formula is:

[0048]

[0049] For the specific structure and implementation process of 2-amino-6-chloropurine, please refer to the relevant discussion in Example 1, and details will not be repeated here.

Embodiment 3

[0051]On the basis of Example 1, this Example 3 provides an intermediate for synthesizing 2-amino-6-chloropurine, whose structural formula is:

[0052]

[0053] For the specific structure and implementation process of the intermediate, please refer to the related discussion of Embodiment 1, which will not be repeated here.

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Abstract

The invention belongs to the technical field of medicines and in particular relates to 2-amino-6-chloropurine as well as a synthesis method, an intermediate and application thereof. The synthesis method of the 2-amino-6-chloropurine comprises the following steps: performing a primary reaction, namely mixing ethyl cyanoacetate, chloroformamidine hydrochloride, liquid ammonia and sodium to implementa reaction so as to generate an intermediate; performing a secondary reaction, namely mixing the intermediate with formic acid to implement a reaction; adding a sodium hydroxide solution into the product of the secondary reaction till alkali; and performing filtering and drying, so as to obtain 2-amino-6-chloropurine. Raw materials are low in price and easy to obtain, reaction steps are small, the reaction time is short, a large amount of wastewater is not generated, and industrial production can be facilitated.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to 2-amino-6-chloropurine and its synthesis method, intermediate and application. Background technique [0002] Famciclovir is the second-generation open-ring nucleotide anti-herpes virus drug, and it is an important variety of current anti-viral oral drugs. After the successful development of Harnden Synthesis in 1985, it was first developed by the British Smith Kline Beecham Company. It was first listed in the UK in 1993, and then successively listed in the United States, Europe and other countries and regions. In 1995, it was approved by the United Kingdom and the United States for genital herpes, and the trade name was Famvi. In 1997, it was approved in the United States for its additional indication - the treatment of recurrent herpes simplex virus infection (genital herpes and cold sores) in HIV patients. This is the first oral drug approved in the United States for the trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/50C07D473/32C07D473/18
CPCC07D239/50C07D473/18C07D473/32
Inventor 吴法浩李钢高仰哲王志航
Owner NANJING REDWOOD FINE CHEM CO LTD
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