Review of Synthetic Approaches toward the Synthesis of Cariprazine, an Antipsychotic Drug

Abstract

Schizophrenia is a chronic and severe mental disorder affecting 20 million people worldwide. Research has not identified the causes of schizophrenia as one single factor. It is thought that interactions between genes and a range of environmental factors may cause schizophrenia. The majority of schizophrenia cases are controlled by the use of antipsychotic drugs, such as aripiprazole, asenapine, olanzapine, quetiapine, risperidone, and cariprazine. Gedeon Richter and Forest Laboratories developed an antipsychotic drug known as cariprazine that contains a piperazine ring, and it is manufactured by Actavis under the trade name Vraylar. This review provides a brief background of the synthetic approaches to cariprazine.

Review on Synthetic Approaches toward the Synthesis of Clozapine, an Antipsychotic Drug

“…In 1976, Josef Schneider et al developed a new method for the synthesis of Clozapine in one step, which is described in US patent US3962248. Clozapine (1) was introduced by using titanium tetrachloride (TiCl 4 ) with 8-chloro-5H-dibenzo[b,e]- [1,4]diazepin-11(10H)-one (8) and N-methylpiperazine (9) in a toluene solvent under reflux conditions for 3 h. After 3 h, isopropyl alcohol was added at 30 °C whereby the insoluble titanium compounds formed during the reaction again dissolved. Subsequently, concentrated ammonia was added (about 27%), cooling is affected to about 30°while stirring, and the resulting precipitate is filtered off.…”

“…In recent years, nitrogen-containing heterocycles playing a vital role whether they are organic or inorganic have been crucial to a variety of biological activities. 1 Due to their remarkable biological characteristics, they are frequently utilized as essential ingredients in the synthesis of several physiologically active compounds. 2 In general, many medicinal drugs employ nitrogen-containing heterocycles, including tricyclic, tetracyclic, pentacyclic, hexacyclic, and heptacyclic, as their core structural components.…”

“…Blunted affect, emotional disengagement, poor rapport, inactivity, difficulties with abstract thought, lack of spontaneity, and stereotypical thinking are some of the negative symptoms. Some of the most often prescribed medications for the treatment of Schizophrenia are Clozapine (1), Risperidone (2), Olanzapine (3), Aripiprazole (4), Cariprazine (5), and Brexpiprazole (6) (Figure 1).…”

“…In recent years, nitrogen-containing heterocycles playing a vital role whether they are organic or inorganic have been crucial to a variety of biological activities . Due to their remarkable biological characteristics, they are frequently utilized as essential ingredients in the synthesis of several physiologically active compounds .…”

Zinc Promoted Urea Synthesis Using Carbonyldiimidazole as Carbonyl Source and Its Application for the Synthesis of Cariprazine

“…Since that date to today‘s modern time urea moieties grabbing the attention of chemists because it plays a significant role in many biologically active natural products, [3] medicines, [4] agrochemicals, [5] material science, [6] and organocatalyst [7] . In addition to this general application urea moieties noted its presence in various drug molecules like Cariprazine, [8] Sorafenib, [9,10] Boceprevir, [11] and Lisuride [12] …”