Nilotinib Powder CAS 641571-10-0

Nilotinib powder is an off-white solid chemical. The molecular formula is C28H22F3N7O, the molecular weight is 529.51600, and the density is 1.36 g/cm3. Nilotinib is an anti-tumor drug, which is a highly selective oral tyrosine kinase inhibitor developed by Novartis Pharmaceutical Company of Switzerland. Its monohydrochloride monohydrate was approved by FDA in October 2007, and its trade name is Tasigna. It is clinically used to treat chronic myeloid leukemia with ineffective imatinib mesylate.

What is Nilotinib?

Nilotinib powder has been used in the clinic. It is a kind of high affinity and multi-target drug. Compared with the first-generation tyrosine kinase inhibitors, the curative effect is greatly improved, the effect is faster, and it has an obvious therapeutic effect on imatinib-tolerant CML patients. Nilotinib has the advantages of high selectivity and few side effects, so it has been approved for clinical treatment, showing its superiority over traditional anti-tumor drugs in treatment, overcoming the shortcomings of poor selectivity and strong adverse reactions in traditional drug treatment, and achieving remarkable clinical treatment effect.

How does Nilotinib work?

(1) synthesis of 3-acetamido -4- methyl -N-[3-(4- methyl -1H- imidazole -1- yl) -5- trifluoromethylphenyl] benzamide (intermediate I):

100g of 3- acetamido-p-toluic acid and 100mL of methylene chloride were put into a dry reaction bottle, then 200mL of thionyl chloride was added with stirring, and then heated and refluxed for 4 hours. After evaporating methylene chloride solvent and excess sulfolane chloride under reduced pressure, 300mL of methylene chloride, 125g of 3-(4- methyl -1H- imidazolyl) -5- trifluoromethylaniline and 108g of triethylamine were put into the residue in the bottle in turn, and the mixture was heated and refluxed for 8 hours. After the reaction, the solvent dichloromethane was distilled off, the residual liquid was poured into 300mL water, yellow solid was precipitated, filtered, and dried to obtain 202g of product with a yield of 93.7%.

(2) Synthesis of 4-methyl -N-[3-(4- methyl -1H imidazolyl) -5- trifluoromethylphenyl ]-3- guanidinobenzamide salt (intermediate II):

45g of 50% aqueous solution of cyanamide, 500mL of ethanol, and I200g of intermediate are put into a reaction bottle, and 245mL of 30% dilute nitric acid is carefully added under stirring, and the reaction is carried out at 20℃ for 20h. At the end of the reaction, 300mL of ice water was added, stirred, and frozen to -5℃, kept for 2 hours, the yellow crystalline solid precipitated by suction filtration, rinsed with a little ice water, and dried to obtain 208g of product with a yield of 90.4%.

(3) Synthesis of nilotinib:

832mL of ethanol, 48g of sodium hydroxide, 76g of 3- dimethylamino -1-(3- pyridyl) -2- propylene -1- one, and 208 g of intermediate II were put into a reaction bottle, and the reaction was heated, stirred and refluxed for 40 hours. At the end of the reaction, cooling to 0℃, crystallizing for 2h, suction filtering, and water washing to obtain nilotinib wet product.

Nilotinib wet product was put into 3 times the weight of ethanol, stirred, and slowly dropped with 35% hydrochloric acid until pH = 2 ~ 3, and after half an hour, the pH remained unchanged. After heating up, dissolving, decolorizing with active carbon, filtering, freezing crystallization, suction filtration, and drying, 202g of product were obtained, with a yield of 88.6% and a purity of 99.86%.

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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure or prevent any disease.

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