Improved and ′Nitrosamines Free′ Process for the Preparation of an α4β2 Neuronal Nicotinic Acetylcholine Receptor Agonist-Varenicline Tartrate was written by Goura, Ramesh;Katari, Naresh Kumar;Ramprasad, A. K.;Rebelli, Pradeep;Surendra Babu, Manabolu Surya. And the article was included in Polycyclic Aromatic Compounds.Application of 230615-52-8 This article mentions the following:
An improvised and efficient approach for synthesis of α4β2 nicotinic acetylcholine receptor subtype agonist, Varenicline tartrate free from the ′N-nitrosamines′ has been described. The approach involves an improved process for a key intermediate (7,8-dinitro-4,5-dihydro-1H-1,5-methanobenzo[d] azepin-3(2H)-yl)-2,2,2-trifluoro ethanone free from potential genotoxic impurities. Compound is converted into Varenicline base in a single pot process with improved overall yield and quality. Further, Varenicline base is converted into Varenicline tartrate by acid addition salt which provides in quant. yield. This improved process consists of tech. innovations/improvements which eliminate the probability for the formation of critical impurities such as dinitro nitroso impurity , diamino nitroso impurity and varenicline nitroso impurity and other genotoxic impurities such as mono nitro impurity and meta dinitro impurity in the final drug substance and provides ′Nitrosamines free′ varenicline tartrate with good quality and yield. In the experiment, the researchers used many compounds, for example, 2,3,4,5-Tetrahydro-1H-1,5-methanobenzo[d]azepine hydrochloride (cas: 230615-52-8Application of 230615-52-8).
2,3,4,5-Tetrahydro-1H-1,5-methanobenzo[d]azepine hydrochloride (cas: 230615-52-8) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. Converting an alcohol to an alkene requires removal of the hydroxyl group and a hydrogen atom on the neighbouring carbon atom. Dehydrations are most commonly carried out by warming the alcohol in the presence of a strong dehydrating acid, such as concentrated sulfuric acid.Application of 230615-52-8
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts