The Production Process of Nintedanib esylate

Nintedanib esylate is a phosphatidylinositol 3-kinase (PI3K) inhibitor used in cancer treatment.
The production process of nintedanib esylate involves several steps, including synthesis, purification, and formulation.
In this article, we will discuss the production process of nintedanib esylate in detail.

Synthesis of Nintedanib Etsylate

The synthesis of nintedanib esylate involves several steps, including the preparation of the starting material, the reaction steps, and the purification process.
The starting material for the synthesis of nintedanib esylate is a substituted aniline, which is reacted with a carbonyl compound in the presence of a palladium catalyst to form a substituted acrylate.
The acrylate is then treated with abase to form an amide, which is then nitrated to form a nitrate.
The nitrate is then treated with a phosphine to form a phosphate, which is finally acylated with a fatty acid to form the final product, nintedanib esylate.

Purification of Nintedanib Etsylate

After the synthesis of nintedanib esylate, the product is typically impure and contains various impurities, such as degradation products, starting materials, and by-products.
Therefore, the purification process is an essential step in the production of nintedanib esylate.
The purification process involves several steps, including crystallization, chromatography, and filtration.

Crystallization is the most common method used for purifying nintedanib esylate.
In this process, the impure product is dissolved in a suitable solvent and allowed to crystallize.
The crystals are then collected and dried to obtain pure nintedanib esylate.

Chromatography is another method used for purifying nintedanib esylate.
In this process, the impure product is passed through a column packed with a stationary phase, such as silica gel or alumina.
The different components of the mixture elute at different rates, allowing for separation and purification of the desired product.

Filtration is also used in the purification process of nintedanib esylate.
In this process, the impure product is passed through a filter to remove any impurities that are insoluble or have a higher molecular weight than the desired product.

Formulation of Nintedanib Etsylate

After the purification process, the final product, nintedanib esylate, is formulated into a dosage form suitable for administration to patients.
The formulation process involves several steps, including milling, blending, compression, and coating.

Milling is the process of grinding the pure nintedanib esylate into a fine powder.
This is necessary for the formation of a uniform dosage form.

Blending is the process of mixing the milled powder with other excipients, such as lactose or mannitol, to form a homogenous mixture.

Compression is the process of forming the mixture into tablets or capsules using a compression machine.
This process is essential for the delivery of the drug to the patient in a consistent and reliable manner.

Coating is the process of applying a thin layer of a polymer or wax to the surface of the tablet or capsule to protect the drug from degradation in the stomach and to improve the patient's acceptance of the dosage form.

Quality Control of Nintedanib Etsylate

Quality control is an essential step in the production process of nintedanib esylate.
This process involves testing the final product for its purity, potency, and stability.
The tests performed include chemical tests, such as testing for the presence of