The Synthetic Routes of Canertinib

Canertinib is a novel tyrosine kinase inhibitor that has shown promise in the treatment of various types of cancer, including lung cancer, colon cancer, and breast cancer.
Its synthetic routes are of great interest to the chemical industry, as they determine the feasibility, efficiency, and cost-effectiveness of its production.
In this article, we will explore the different synthetic routes of Canertinib and their potential applications in the chemical industry.

1. Hydrogenation of 4-Chloro-3-nitrophenyl Acetate

One of the most commonly used synthetic routes for Canertinib involves the hydrogenation of 4-chloro-3-nitrophenyl acetate.
This reaction involves the addition of hydrogen gas to 4-chloro-3-nitrophenyl acetate in the presence of a metal catalyst, such as palladium or platinum.
The resulting product is then purified and further processed to produce Canertinib.
This route is relatively simple and efficient, and can be used to produce large quantities of Canertinib at a reasonable cost.

2. Condensation of 2-Amino-6-Chloropurine and 4-Amino-3-Nitrophenol

Another synthetic route for Canertinib involves the condensation of 2-amino-6-chloropurine and 4-amino-3-nitrophenol.
This reaction involves the condensation of the two amino compounds in the presence of a strong acid catalyst, such as sulfuric acid.
The resulting product is then purified and further processed to produce Canertinib.
This route is also relatively simple and efficient, and can be used to produce high-quality Canertinib at a reasonable cost.

3. Reduction of 4-Chloro-3-nitrophenyl Ether

Canertinib can also be synthesized through the reduction of 4-chloro-3-nitrophenyl ether.
This reaction involves the reduction of the ether compound using a reducing agent, such as lithium aluminum hydride or hydrogen in the presence of a metal catalyst, such as nickel or palladium.
The resulting product is then purified and further processed to produce Canertinib.
This route is more complex than the previous two routes, but can still be used to produce Canertinib at a reasonable cost.

4. Semi-Synthetic Route

A semi-synthetic route for Canertinib involves the synthesis of the phosphate group and the sulfonamide group, which are then condensed to form Canertinib.
This route is more complex than the previous routes, but can be used to produce Canertinib at a lower cost than other synthetic routes.

In conclusion, there are various synthetic routes for Canertinib, each with its own advantages and disadvantages.
The hydrogenation of 4-chloro-3-nitrophenyl acetate and the condensation of 2-amino-6-chloropurine and 4-amino-3-nitrophenol are the most commonly used routes and are suitable for large-scale production.
The reduction of 4-chloro-3-nitrophenyl ether is more complex but can still be used to produce Canertinib at a reasonable cost.
The semi-synthetic route can be used to produce Canertinib at a lower cost than other routes.
Ultimately, the choice of synthetic route for Canertinib will depend on the needs of the chemical industry and the desired cost and production efficiency.