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An improvised and efficient approach for synthesis of α4β2 nicotinic acetylcholine receptor subtype agonist, Varenicline tartrate ( 1 ) 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 ( 7 ) free from potential genotoxic impurities. Compound  7  is converted into Varenicline base  10  in a single pot process with improved overall yield and quality. Further, Varenicline base  10  is converted into Varenicline tartrate ( 1 ) by acid addition salt which provides in quantitative yield. Our improved process consists of technical innovations/improvements which eliminate the probability for the formation of critical impurities such as dinitro nitroso impurity  2 , diamino nitroso impurity  3  and varenicline nitroso impurity  4  and other genotoxic impurities such as mono nitro impurity  11  and meta dinitro impurity  12  in the final drug substance and provides ‘Nitrosamines free’ varenicline tartrate ( 1 ) with good quality and yield.

Improved and ‘Nitrosamines Free’ Process for the Preparation of an α4β2 Neuronal Nicotinic Acetylcholine Receptor Agonist-Varenicline Tartrate