The Synthetic Routes of Lurasidone

Lurasidone is an atypical antipsychotic agent that is used to treat schizophrenia and bipolar disorder.
It is a benzisoxazole derivative that contains a substituted dibenzoxazepine structure, and it is known for its potent and long-lasting antipsychotic effects.
Lurasidone was first synthesized by Taro Pharmaceutical Industries Ltd.
, and it was approved by the U.
S.
Food and Drug Administration (FDA) in 2010 under the brand name Latuda.

There are several synthetic routes for the preparation of lurasidone, but the most commonly used route involves the condensation of an aromatic aldehyde with 4-chloro-2-methyl-6-phenyl-1,3-oxazepane in the presence of a strong base.
This reaction results in the formation of 1,3-oxazepan-4-one, which is then treated with sodium hydride and an aromatic amine in the presence of a solvent such as N-methyl-2-pyrrolidone (NMP) to form the final product.

Another synthetic route for the preparation of lurasidone involves the condensation of an aromatic aldehyde with 4-methyl-6-phenyl-1,3-oxazepane in the presence of a Lewis acid catalyst such as boron trifluoride (BF3).
This reaction is followed by treatment with sodium hydride and an aromatic amine in the presence of a solvent such as NMP to form the final product.

A third synthetic route for the preparation of lurasidone involves the condensation of an aromatic aldehyde with 4-methyl-6-phenyl-1,3-oxazepane in the presence of hydrochloric acid, followed by treatment with sodium hydride and an aromatic amine in the presence of a solvent such as NMP to form the final product.

The choice of synthetic route for the preparation of lurasidone depends on several factors, including the availability and cost of the starting materials, the desired yield and purity of the product, and the scale of production.
Each of the synthetic routes described above has its own advantages and disadvantages, and the selection of the most appropriate route should be based on a careful consideration of these factors.

In conclusion, lurasidone is an important antipsychotic agent that is used to treat schizophrenia and bipolar disorder.
There are several synthetic routes for the preparation of lurasidone, and the choice of route depends on several factors.
The synthetic routes described above involve the condensation of an aromatic aldehyde with 4-methyl-6-phenyl-1,3-oxazepane, followed by treatment with sodium hydride and an aromatic amine in the presence of a solvent such as N-methyl-2-pyrrolidone (NMP) or hydrochloric acid.
The choice of synthetic route depends on the availability and cost of the starting materials, the desired yield and purity of the product, and the scale of production.