TAILIEUCHUNG - Solvent-free microwave-assisted synthesis of aripiprazole

Aripiprazole is a widely used antipsychotic approved by the FDA (Food and Drug Administration) in 2002. Methods for preparation of aripiprazole mainly involve the use of expensive and toxic solvents, and the reaction time can be even several hours long. | Solvent-free microwave-assisted synthesis of aripiprazole Current Chemistry Letters 7 2018 81 86 Contents lists available at GrowingScience Current Chemistry Letters homepage Solvent-free microwave-assisted synthesis of aripiprazole Jolanta Jaśkowskaa Anna K. Drabczyka Damian Kułagaa Przemysław Zarębaa and Zbigniew Majkab a Faculty of Chemical Engineering and Technology Institute of Organic Chemistry and Technology Cracow University of Technology 24 Warszawska Street 31-155 Cracow Poland b TM Labs 14 Bieliny-Prażmowskiego Street 31-514 Cracow Poland CHRONICLE ABSTRACT Article history Aripiprazole is a widely used antipsychotic approved by the FDA Food and Drug Received April 28 2018 Administration in 2002. Methods for preparation of aripiprazole mainly involve the use of Received in revised form expensive and toxic solvents and the reaction time can be even several hours long. Our method June 29 2018 allows to obtain aripiprazole with a yield of approximately 70 80 over just a few minutes Accepted August 12 2018 using solvent-free conditions in the presence of PTC Phase Transfer Catalysts and microwave Available online August 12 2018 radiation. Keywords Solvent-free synthesis Microwave-assisted synthesis PTC catalysts Aripiprazole Long Chain Arylpiperazines LCAPs 2018 Growing Science Ltd. All rights reserved. 1. Introduction The antipsychotic efficacy of aripiprazole 1 is due to its activity as a partial agonist of dopamine D2 and serotonin 5-HT1A receptors and antagonist of a 5-HT2A serotonin receptor Fig. 1 . Aripiprazole 1 is recommended for the treatment of schizophrenia and manic episodes. H O N O N Cl N Cl Fig. 1. Structure of aripiprazole 1 The most widely described in the literature synthetic route of aripiprazole 1 is a reaction between 7- 4-halobutoxy -3 4-dihydrocarbostyril BBQ and 1- 2 3-dichlorophenyl piperazine DCP in the presence of bases such as triethylamine 1-3 pyridine sodium hydroxide or hydride 1 4 potassium 1 4-13 .

• Hoá học
• Long Chain Arylpiperazines
• Solvent free synthesis
• Microwave assisted synthesis
• Food and Drug Administration
• Phase Transfer Catalysts
• Journal of Chemistry
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• New optically active bis quaternary ammonium salts
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