General Information

Varenicline Impurities and Varenicline 

Daicel Pharma is a reliable partner for synthesizing high-quality Varenicline impurities, specifically 1-((1R,5S)-8-amino-6-nitro-1,2,4,5-tetrahydro-3H-1,5-methanobenzo[d]azepin-3-yl)-2,2,2-trifluoroethan-1-one, Methyl Varenicline Impurity, N-Nitroso Varenicline, Varenicline Impurity II, Trifluoroacetyl Varenicline Hydroxymethyl Impurity, Varenicline tartrate adduct and more. These impurities help assess the quality, stability, and safety of the active pharmaceutical ingredient, Varenicline. Daicel Pharma also offers custom synthesis of Varenicline impurities, which can be shipped worldwide.

Varenicline [CAS: 249296-44-4] is a medication that acts as a partial agonist of the nicotinic acetylcholine receptor, alpha4beta2. It helps in giving up smoking.

Varenicline: Use and Commercial Availability  

Varenicline is an organic compound similar to cytisine that acts as a partial agonist for nicotinic cholinergic receptors. It is available in its tartrate salt form. Varenicline helps as a smoking cessation aid, with patients undergoing education and counseling in conjunction with its use. It is considered the first line of treatment for smoking cessation due to its ability to prevent short-term and long-term relapse. Varenicline appears more effective than bupropion and equally effective as nicotine replacement therapy. Additionally, Varenicline has a lower risk of withdrawal symptoms due to its partial agonist properties. Some of the brand names for Varenicline include Chantix and Tyrvaya.

Varenicline Structure and Mechanism of Action

The chemical name of Varenicline is 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine. Its chemical formula is C₁₃H₁₃N₃, and its molecular weight is approximately 211.26 g/mol.

Varenicline binds selectively and with affinity at α₄β₂ neuronal nicotinic acetylcholine receptors. It ends smoking in patients and prevents nicotine binding at α₄β₂ receptors.

Varenicline Impurities and Synthesis

During the synthesis¹ and storage of Varenicline, impurities may form that can affect the drug’s safety and efficacy. Some impurities include related substances, starting materials, and degradation products. The impurity control is through proper process development, purification, and storage conditions.

Daicel Pharma issues a Certificate of Analysis (CoA) for Varenicline impurity standards, including 1-((1R,5S)-8-amino-6-nitro-1,2,4,5-tetrahydro-3H-1,5-methanobenzo[d]azepin-3-yl)-2,2,2-trifluoroethan-1-one, Methyl Varenicline Impurity, N-Nitroso Varenicline, Varenicline Impurity II, Trifluoroacetyl Varenicline Hydroxymethyl Impurity, Varenicline tartrate adduct and more. The CoA is from an analytical facility that complies with current Good Manufacturing Practices (cGMP) and includes comprehensive characterization data, such as 1H NMR, 13C NMR, IR, MASS, and HPLC purity². We give additional characterization data such as 13C-DEPT and CHN on request. Daicel Pharma can prepare unknown Varenicline impurities or degradation products. A complete characterization report accompanies each delivery.