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Usage

Uses

Used in Pharmaceutical Industry:
8-(2,3-Dichlorophenyl)-8-aza-5-azoniaspiro[4.5]decane Bromide is used as a key intermediate in the synthesis of Aripiprazole (A771000), a selective dopamine D2-receptor antagonist with dopamine autoreceptor agonist activity. This medication is widely prescribed for the treatment of various psychiatric disorders, including schizophrenia, bipolar disorder, and major depressive disorder.
As an Antipsychotic:
8-(2,3-Dichlorophenyl)-8-aza-5-azoniaspiro[4.5]decane Bromide contributes to the development of Aripiprazole, an antipsychotic agent that helps in managing the symptoms of psychotic conditions by modulating the dopamine levels in the brain. Its unique mechanism of action allows for a more targeted approach to treatment, reducing the risk of side effects commonly associated with traditional antipsychotics.
In the Production of Aripiprazole Impurity 12:
8-(2,3-Dichlorophenyl)-8-aza-5-azoniaspiro[4.5]decane Bromide is also utilized in the preparation of Aripiprazole Impurity 12, which is an important component in the quality control and manufacturing processes of Aripiprazole. The presence of this impurity helps in ensuring the purity and efficacy of the final drug product, as well as in the development of analytical methods for its detection and quantification.

Upstream product

• 119532-26-2 1-(2,3-dichlorophenyl)-piperazine hydrochloride 
• 110-52-1 1,4-dibromo-butane 

Downstream Products

• 129722-12-9 aripiprazole 

Relevant academic research and scientific papers

Preparation method of aripiprazole

The invention discloses a preparation method of aripiprazole. The method comprises the following steps: dissolving 1-(2,3-dichlorophenyl)piperazine or a salt thereof in a polar solvent, adding 1,4-dibromobutane and an acid binding agent, carrying out a reaction under a first heating condition, performing first cooling and first filtration to obtain a first filtrate, distilling the solvent out of the first filtrate, adding a weakly polar solvent for crystallization, performing second filtration to obtain a second filtrate, performing drying to obtain 1-(2,3-dichlorophenyl)piperazine azacyclopentamine salt, adding the 1-(2,3-dichlorophenyl)piperazine azacyclopentamine salt, 7-hydroxyl-3,4-dihydroquinolone, and an alcohol base in an anhydrous alcohol, carrying out a reaction under a second heating condition, performing second cooling, performing dispersing by pouring the cooled system into ice water, performing third filtration, performing washing with water, and performing crystallization to obtain aripiprazole. According to the provided method, the process raw materials are easy to obtain, the route is simple and short, and the high-purity target product can be obtained. Compared with a method of the prior art, the method optimizes the process conditions, reduces the production cost, has good product quality, has high yield, and is favorable for industrialized production.

PROCESS FOR THE PREPARATION OF CARBOSTYRIL DERIVATIVES, SUCH AS ARIPIPRAZOLE AND ITS INTERMEDIATES

A process for preparing carbostyril derivatives such as aripiprazole is described. Dichlorophenylpiperazine or an acid addition salt thereof is reacted with a compound of formula X-C4H8-Y or X-C4H6-Y to produce a novel quaternary spiro ammonium salt intermediate which is optionally isolated and purified. The quaternary spiro ammonium salt intermediate is reacted with 7-hydroxydihydrocarboxystyryl to produce the carbostyril derivative.