230615-69-7Relevant articles and documents
Varenicline: An α4β2 nicotinic receptor partial agonist for smoking cessation
Coe, Jotham W.,Brooks, Paige R.,Vetelino, Michael G.,Wirtz, Michael C.,Arnold, Eric P.,Huang, Jianhua,Sands, Steven B.,Davis, Thomas I.,Lebel, Lorraine A.,Fox, Carol B.,Shrikhande, Alka,Heym, James H.,Schaeffer, Eric,Rollema, Hans,Lu, Yi,Mansbach, Robert S.,Chambers, Leslie K.,Rovetti, Charles C.,Schulz, David W.,Tingley III, F. David,O'Neill, Brian T.
, p. 3474 - 3477 (2005)
Herein we describe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine) has been identified for smoking cessation. Neuronal nicotinic acetylcholine receptors (nAChRs) mediate the dependence-producing effects of nicotine. We have pursued α4β2 nicotinic receptor partial agonists to inhibit dopaminergic activation produced by smoking while simultaneously providing relief from the craving and withdrawal syndrome that accompanies cessation attempts. Varenicline displays high α4β2 nAChR affinity and the desired in vivo dopaminergic profile.
Hydrogenation of a pharmaceutical intermediate by a continuous stirred tank reactor system
Van Alsten, John G.,Jorgensen, Matthew L.,Am Ende, David J.
, p. 629 - 633 (2009)
A proof of concept study on the continuous hydrogenation of a pharmaceutical intermediate is presented. A slurry feed of CP- 548495, a dintro intermediate in a smoking cessation drug, was reduced in a two-reactor continuous stirred tank train to the diami
Cocrystal of varenicline and oxalic acid, pharmaceutical composition thereof, and methods of use thereof
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Page/Page column 8-9, (2021/06/23)
Provided is a cocrystal of varenicline and oxalic acid. In particular, provided is a cocrystal of varenicline and oxalic acid of formula (I) having a molar ratio of varenicline to oxalic acid of 1:1.5. Also provided is a process for preparing the cocrystal, a pharmaceutical composition containing the cocrystal and a method of using the cocrystal and pharmaceutical composition, such as for reducing nicotine addiction or tobacco use.
AN IMPROVED PROCESS FOR THE PREPARATION OF VARENICLINE AND SALT THEREOF
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, (2018/09/28)
of the Invention The present invention relates to an improved process for the preparation of varenicline and salt thereof. The present invention also provides a process for the 2,7preparation of l-(4,5-dinitro-10-aza-tricyclo[6.3.1.0 ]dodeca-2(7),3,5-trien-10-yl)-2,2,2-trifluoroethanone of Formula 4 using ethyl trifluoroacetate and further converted to varenicline and salt thereof.