- PROCESS FOR PREPARING VARENICLINE, VARENICLINE INTERMEDIATES, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Provided herein is an improved, convenient, commercially viable and environmentally friendly process for the preparation of varenicline or a pharmaceutically acceptable salt thereof comprising reacting l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien- 10-yl)-2,2,2-trifluoro-ethanone with chloroacetaldehyde in the pressence of an oxygen source. Provided further herein is an improved and industrially advantageous process for the preparation of l-(4,5-diamino-10-aza-tricyclo[6.3.1.02 7]dodeca-2(7),3,5-trien-10-yl)-2,2,2- trifluoro-ethanone.
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Page/Page column 17
(2010/04/06)
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- IMPROVED PROCESSES FOR THE SYNTHESIS OF VARENICLINE L-TARTRATE
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This invention provides a process of preparing varenicline L-tartrate salt. This invention also provides varenicline L-tartrate produced by the instant method, as well as a pharmaceutical composition comprising same.
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Page/Page column 11-12
(2009/06/27)
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- PROCESSES FOR THE PREPARATION OF VARENICLINE AND INTERMEDIATES THEREOF
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The invention provides an improved process for the preparation and purification of Varenicline and intermediates for the preparation of Varenicline.
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Page/Page column 9-10
(2009/12/28)
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- 3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation
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3,5-Bicyclic aryl piperidines are a new class of high-affinity α4β2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the α4β2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic dopamine system, a key measure of therapeutic potential for smoking cessation.
- Coe, Jotham W.,Brooks, Paige R.,Wirtz, Michael C.,Bashore, Crystal G.,Bianco, Krista E.,Vetelino, Michael G.,Arnold, Eric P.,Lebel, Lorraine A.,Fox, Carol B.,Tingley III, F. David,Schulz, David W.,Davis, Thomas I.,Sands, Steven B.,Mansbach, Robert S.,Rollema, Hans,O'Neill, Brian T.
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p. 4889 - 4897
(2008/12/23)
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- Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic componunds
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The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: wherein R1, R2, R3, R4, and R5 are defined herein. Compounds of formulae (Ia), (Ib) and (IC) or mixtures thereof are useful in the preparation of compounds of formula (II): wherein R2, R3 and R6 are also defined herein.
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- Aryl fused azapolycyclic compounds
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Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, R3 and n are defined as in the specification, intermediates in the synthesis of such compounds, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of neurological and psychological disorders are claimed.
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