Method for preparing 2,3-dihydro-1H-pyrrolo pyridine hydrochloride

A pyrrole and pyridine technology, applied in the field of new preparation of pharmaceutical intermediates, can solve problems such as unreasonable application, multi-drug resistance, abuse, etc.

Inactive Publication Date: 2014-12-24
湖南华腾制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are many kinds of antimicrobial drugs in clinical use, but with the large number of antimicrobial drugs, they are widely used, especially in clinical irrational application, even abuse, and finally lead to multi-drug resistance

Method used

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  • Method for preparing 2,3-dihydro-1H-pyrrolo pyridine hydrochloride
  • Method for preparing 2,3-dihydro-1H-pyrrolo pyridine hydrochloride
  • Method for preparing 2,3-dihydro-1H-pyrrolo pyridine hydrochloride

Examples

Experimental program
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Effect test

Embodiment 1

[0022] (1) Synthesis of 2H-pyrrolo[3,4-c]pyridine-1,3-dione

[0023] Add 30g of furo[3,4-c]pyridine-1,3-dione into 180ml of o-xylene, add 25g of urea, heat, stir and reflux for 6 hours, cool to room temperature, filter, then add water and ethyl acetate Extraction, liquid separation, drying, and concentration were performed to obtain a crude product, which was passed through a column to obtain recrystallization to obtain 16 g of 2H-pyrrolo[3,4-c]pyridine-1,3-dione.

[0024] (2) Synthesis of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine

[0025] Add 15g of 2H-pyrrolo[3,4-c]pyridine-1,3-dione into 150ml of tetrahydrofuran, cool down to 0°C, add 6.5g of lithium aluminum tetrahydride in batches under a nitrogen atmosphere, after the addition, 0 React at ℃ for 1 hour, then slowly rise to room temperature and stir overnight, add 1N hydrochloric acid, then add ethyl acetate, extract and separate, collect the organic phase, separate, dry and concentrate, and the residue is separated on a sili...

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Abstract

The invention discloses a method for preparing 2,3-dihydro-1H-pyrrolo-[3,4-c] pyridine hydrochloride. A target product is obtained through lactamization, reduction and salification by taking furo[3,4-c] pyridine-1,3-dione as an initial raw material, and the compound is an important medical intermediate.

Description

technical field [0001] The invention relates to a novel preparation method of a pharmaceutical intermediate, in particular to a preparation method of 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine hydrochloride. technical background [0002] Compound 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine hydrochloride, the structural formula is: [0003] [0004] Antimicrobial drugs are a class of drugs that are widely used in clinical practice and used in large doses, and play an important role in the control and treatment of diseases. At present, there are many kinds of antimicrobial drugs in clinical use, but with the large number of antimicrobial drugs, they are widely used, especially in clinical irrational application, and even abuse, which eventually leads to multi-drug resistance. Therefore, how to overcome multi-drug resistance has become an important topic of antimicrobial drug research at home and abroad. There are many ways to solve drug resistance, and the research and development o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 邓泽平陈芳军李书耘
Owner 湖南华腾制药有限公司
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