Polycyclic carbamoyl pyridone analogue and preparation method and application thereof

A technology of polycyclic carbamoyl pyridone and cyclic carbamoyl pyridone, which is applied in the field of medicinal chemistry, can solve the problems of poor patient compliance, slow onset time and the like, achieves good functional group tolerance, the method is simple to operate, and the process Economical effect

Active Publication Date: 2021-04-20
CHONGQING MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Drugs such as oseltamivir, zanamivir, amantadine and rimantadine are currently widely used anti-influe

Method used

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  • Polycyclic carbamoyl pyridone analogue and preparation method and application thereof
  • Polycyclic carbamoyl pyridone analogue and preparation method and application thereof
  • Polycyclic carbamoyl pyridone analogue and preparation method and application thereof

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[0032]Example 1

[0033]The formula I compound, chlorolymentaldehyde, and 1,4-dioxidin were added to a dry clean reaction bottle, and the mixture was stirred to 100 ° C for 5 h after 5 h, and the sodium hydrogencarbonate continued to react, TLC point plate monitoring reaction is complete, pending system It was cooled to room temperature, adding water / ethyl acetate extraction 3 times, combined with organic phases, washed with saturated brine, and collected, dried over anhydrous sodium sulfate, filtered, concentrated under reduced pressure, residue was purified to obtain a target product.

[0034]In the initial experiment, the inventors conducted 2-amino-N- (2-hydroxyethyl) benzamide and chlorohydecethemical synthesis 3, 4, 11, 11a-tetrahydrogen - [1,4] loinzine [3,4-B] Quinazoline-6 ​​(1H) - the reaction conditions of ketone, the results are shown in Table 1. First tried the reaction conditions are Nahco3(1.2 equivalents) as a catalyst, at 1,4-dioxanes to be a solvent 100 ° C for 8 h. It...

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Abstract

The invention provides a polycyclic carbamoyl pyridone analogue which is used as a polycyclic carbamoyl pyridone analogue and can be used as a medicine raw material or an intermediate for synthesizing a novel anti-influenza virus medicine. The polycyclic carbamoyl pyridone analogue is obtained by cyclization of the o-amino amide derivative and chloroacetaldehyde under the action of alkali without any other catalyst or additive, harsh reaction conditions are not needed, and the method is simple to operate and suitable for industrial production. The invention also discloses application of the polycyclic carbamoyl pyridone analogue in serving as an impurity reference substance of baloxavir dipivoxil analogue drugs.

Description

technical field [0001] The invention relates to a polycyclic carbamoyl pyridone, in particular to a polycyclic carbamoyl pyridone analogue and its preparation method and use, belonging to the technical field of medicinal chemistry. Background technique [0002] Influenza is an acute respiratory infectious disease caused by influenza virus. It has the characteristics of wide prevalence, strong infectivity, and high incidence. At present, vaccination and drug treatment are the main measures to deal with influenza virus infection. However, vaccination is difficult to effectively immunize high-risk groups such as the elderly and children, and at the same time cannot provide extensive and durable immune protection for the body; in addition, the continuous evolution of influenza virus strains and the emergence of new virus strains have greatly reduced the effectiveness of vaccines. sex. Therefore, drug treatment is still the best means of controlling the spread of influenza viru...

Claims

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Application Information

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IPC IPC(8): C07D498/04C07D498/14
Inventor 袁建勇王强胡雪原吴惠丽匡秋林
Owner CHONGQING MEDICAL UNIVERSITY
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