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Erlotinib hydrochloride is a widely used cancer treatment drug that belongs to the class of tyrosine kinase inhibitors.
It is commonly used to treat non-small cell lung cancer, pancreatic cancer, and ovarian cancer.
The synthesis of erlotinib hydrochloride has been extensively studied in the chemical industry, and there are several synthetic routes available to produce this compound.
One of the most commonly used synthetic routes for erlotinib hydrochloride involves a sequence of reactions that starts with the synthesis of the starting material, 2-aminonaphthalene.
This compound is then converted into the intermediate 2-aminofluorene through a reaction with chloroform and subsequent treatment with hydroxylamine.
The intermediate is then transformed into the naphthalene derivative 1-naphthylamine through a reaction with hydrazine.
The final step in this synthetic route involves the treatment of 1-naphthylamine with hydrochloric acid to produce erlotinib hydrochloride.
Another synthetic route for erlotinib hydrochloride involves the use of a precursor compound, CPP-770.
This compound is treated with chloroform and then hydroxylated to produce the intermediate 7-hydroxymethyl-2-oxo-1,2,3,4-tetrahydroquinoline-3-carboxylic acid.
This intermediate is then transformed into the desired product through a series of reactions, including reduction, alkylation, and hydrolysis.
In another synthetic route, erlotinib hydrochloride is synthesized by treating 2-aminoanthraquinone with chloroform and then hydroxylating the resulting intermediate to produce 2,3-dihydro-1H-benz[de]anthracen-7-one.
This compound is then treated with chloroform and hydroxylated again to produce the desired product.
The choice of synthetic route for erlotinib hydrochloride depends on several factors, including the availability of starting materials, the cost of the synthesis, and the desired yield of the product.
The synthetic routes described above are just a few examples of the many methods that have been developed for the synthesis of erlotinib hydrochloride.
The production of erlotinib hydrochloride on an industrial scale typically involves a multi-step synthetic route that involves several purification steps to ensure the purity of the final product.
The synthetic route is usually designed to maximize the yield of the desired product while minimizing the formation of side products.
The final product is then formulated into the desired dosage form, such as a tablet or capsule, and packaged for distribution to pharmacies and hospitals.
In conclusion, the synthetic routes of erlotinib hydrochloride involve a series of chemical reactions that convert starting materials into the desired product.
The choice of synthetic route depends on various factors, and the production of erlotinib hydrochloride on an industrial scale involves several purification steps and a multi-step synthetic route.
The development of new and more efficient synthetic routes for erlotinib hydrochloride remains an active area of research in the chemical industry, with the goal of improving the efficiency and cost-effectiveness of the synthesis of this important cancer treatment drug.