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New use of 4, 5-disubstituted-2-pyrrolidone compound

A technology of pyrrolidone and compound, applied in the field of pharmaceutical application, can solve the problems of forgetfulness, toxic and side effects, bone marrow suppression and the like

Inactive Publication Date: 2014-06-25
THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The clinical application of these drugs prolongs the lives of AIDS patients, but it is also accompanied by serious side effects, such as bone marrow suppression, amnesia and the occurrence of drug resistance

Method used

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  • New use of 4, 5-disubstituted-2-pyrrolidone compound
  • New use of 4, 5-disubstituted-2-pyrrolidone compound
  • New use of 4, 5-disubstituted-2-pyrrolidone compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation of 4,5-disubstituted-2-pyrrolidone compound (ie general formula I):

[0039] The preparation of trans 4-phenyl-5-o-chlorobenzyl-2-pyrrolidone is according to the invention patent ZL97123419.1 (d1-trans-4-phenyl-5-o-chlorobenzylpyrrolidone-2 synthesis process) The disclosed method, the synthetic route is as follows:

[0040]

[0041] (1) Synthesis of 2-o-chlorophenylnitroethylene (intermediate IV)

[0042] Method A: Mix 8g of o-chlorobenzaldehyde (0.057mol) and nitromethane (5.2g, 0.086mol) in 25ml of methanol, add 10% KOH aqueous solution dropwise under stirring at 0-5°C to adjust the pH of the reaction solution to 8-9, continue to react for 2 hours (check the reaction process by TLC), add dropwise 10% KOH aqueous solution to adjust the pH to greater than 10, and react for 30 minutes, quickly pour the reaction solution into ice water with concentrated hydrochloric acid, stir for 30 minutes, add A certain amount of saturated saline, the precip...

Embodiment 2

[0051] Example 2: Take (dl)-trans-4-phenyl-5-o-chlorobenzyl-2-pyrrolidone, grind it through an 80-mesh sieve, add appropriate amount of starch, dextrin, and lactose and mix evenly , granulated, dried, granulated, and divided into capsule shells to obtain capsules. The preparation is orally administered twice a day, and the dose of each dose is 5-100 mg based on the raw material drug.

Embodiment 3

[0052] Example 3: Take 4-phenyl-5-benzyl-2-pyrrolidone, crush it and pass through an 80-mesh sieve, add appropriate amount of starch, dextrin, and lactose, mix evenly by equal multiplication method, granulate, dry, and granulate. The granules are compressed into tablets. The preparation is orally administered twice a day, and the dose of each dose is 5-100 mg based on the raw material drug.

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Abstract

The invention discloses application of a 4, 5-disubstituted-2-pyrrolidone compound in preparation of anti-AIDS drugs and preparation of reverse transcriptase inhibitor drugs. Test on the anti-HIV-1 activity of the compound provided by the invention by an international general experimental method finds that the compound has good anti-HIV-1 activity, small toxic and side effect, and has good new drug development prospects.

Description

technical field [0001] The invention relates to the medicinal application of 4,5-disubstituted-2-pyrrolidone compound, in particular the application as a reverse transcriptase inhibitor in the preparation of anti-AIDS drugs, and belongs to the technical field of pharmaceutical application. Background technique [0002] AIDS (Acquired Immuno-deficiency Syndrome, AIDS) is an acquired immune deficiency syndrome, which is one of the incurable diseases that threaten human health in the world today. The pathogen that causes AIDS is Human Immunodeficiency Virus (HIV). There are two subtypes of HIV, HIV-1 and HIV-2, and several variants. The development of anti-AIDS drugs mainly focuses on HIV reverse transcriptase (RT) inhibitors, protein synthetase inhibitors, reverse transcription initiation factor inhibitors, etc., and has successfully developed reverse transcriptase inhibitors (such as AZT, DDC, DDI, D4T, etc.) and protease inhibitory drugs (such as Ritonavir, Indinavir, Nelfi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4015A61P31/18
Inventor 杨小生郑永唐郝小江汪冶
Owner THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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