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Process for preparing ropinirole and its salt

A technology for ropinirole hydrochloride and a compound is applied in the field of preparation of ropinirole and its salts, and achieves the effects of strong controllability, mild reaction conditions and simple operation

Inactive Publication Date: 2009-11-18
北京德众万全医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In this type of synthetic method, dangerous reagents such as Raney nickel (WO9415918) are used, or expensive reagents such as palladium carbon (J.Heterocyclic Chem., 32,875 (1995); EP 0300614 (CN1030076A)) are used, or Uncommon reagent MeSCH 2 CO 2 Me (WO 9415918), etc., all have certain production limitations

Method used

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  • Process for preparing ropinirole and its salt
  • Process for preparing ropinirole and its salt
  • Process for preparing ropinirole and its salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The preparation of embodiment 1 ropinirole hydrochloride

[0018] 38 grams of intermediate I, 100 milliliters of water, 300 milliliters of 95% ethanol and 280 grams of zinc powder were mixed and stirred. Raise the temperature to reflux for 4 hours, then heat filter to remove unreacted zinc sludge and zinc oxide produced by the reaction. 20 ml of concentrated hydrochloric acid was added to the filtrate to reflux for 2 hours, most of the ethanol was evaporated from the reaction solution under reduced pressure, and the residue was decolorized with activated carbon. Filter, cool the filtrate, and adjust the pH value to 8-9 with sodium hydroxide solution. Dichloromethane extraction, 200 milliliters of isopropanol and 20 milliliters of concentrated hydrochloric acid were added to the extract, most of the solvent was evaporated under reduced pressure, the residue was cooled at room temperature, and a yellow solid was precipitated, which was filtered to obtain 18 grams of a li...

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Abstract

The invention relates to a process for preparing Ropinirole and its salts.

Description

field of invention [0001] The invention relates to a preparation method of ropinirole and a salt thereof. Background of the invention [0002] Ropinirole (as shown in formula II) is an early-stage Parkinson's disease treatment drug developed by the British Smith K Line-Beecham Pharmaceutical Company. It was first listed in the UK in 1996, and was subsequently listed in France, Switzerland and other countries. [0003] [0004] Ropinirole [0005] Ropinirole is a potent, selective non-ergot alkaloid dopamine D 2 -A receptor agonist, which can directly stimulate striatal dopamine receptors, has similar early efficacy to L-dopamine in young patients, is well tolerated, and has a small dose. At present, the domestic development of this drug has a good market prospect. There are two main methods for the synthesis of ropinirole, one is to form an indole ring first, and then dock with di-n-propylamine. In this type of synthetic method, dangerous reagents such as Raney nickel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/34
Inventor 刘昆张志强高雪松
Owner 北京德众万全医药科技有限公司
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