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.
The present work provides a fast and mild method towards the synthesis of urea derivatives and their application in amino group protection. This new methodology is an inexpensive, simple, and environmentally safe process for the synthesis of urea derivatives. It is well suited for aliphatic amines and aromatic amines. With aliphatic amines, Zn-mediated urea bond formation occurs at ambient temperature, whereas with aromatic amines, it occurs at 60 °C. Environmentally friendly reaction conditions, sustainability, enumerating tolerance of a wide variety of functional groups, cost-effectiveness, high atom economy, fast reaction time, and adaptability for large-scale synthesis are all benefits of this technology.
Herein, we report a synthetic protocol for the synthesis of carbamates by employing zinc chloride as a catalyst from carbamoyl chlorides and aromatic/aliphatic alcohols. The developed protocol successfully utilizes the gram-scale synthesis of the FDA-approved rivastigmine drug and its derivative. The utility of zinc chloride over other catalysts such as zinc dust and zinc acetate exhibits a 49−87% yield of carbamates.
A convenient method has been developed for symmetrical and un‐symmetrical urea synthesis by using Carbonyldiimidazole (CDI) and recyclable activated zinc metal. This reaction is suitable for all types of amines and gives the desired urea products with good to excellent yield. The developed synthetic approach was employed for the synthesis of the Cariprazine drug.
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