- COCRYSTAL OF VARENICLINE AND OXALIC ACID, PHARMACEUTICAL COMPOSITION THEREOF, AND METHODS OF USE THEREOF
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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.
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- Preparation method of vanniklan tartrate tablets degraded impurities
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The present invention proposes a method for the preparation of the degradation of impurities in the tartaric acid vareniclan tablets, with ammonium formate as a hydrogen donor, the dinitrolate is reduced under the palladium carbon catalyzed to obtain a diamidylation, the diaminolide and the aqueous solution of glyal are cyclic reaction to obtain a cyclic product, and then the cyclic product is hydrolyzed under the action of sodium hydroxide, the trifluoroacetyl group is removed to obtain a free base, and finally the free base is reacted with chloroacetic acid under the action of the alkali, and the solvent is evaporated after the end of the reaction, Add water to dissolve and adjust the pH until the solids precipitate from the aqueous phase, collect and filter the solids to dry to obtain acetic acid adducts. The present invention fills the technical gap of the current impurity preparation method, the prepared high-purity impurities can be applied as a control sample to the pharmaceutical impurity research and production quality control process of varenicline tartrate, providing a guarantee for the comprehensive quality control of the varenicline tartrate API.
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- Cocrystal of varenicline and oxalic acid, pharmaceutical composition thereof, and methods of use thereof
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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.
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Page/Page column 8-9
(2021/06/23)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF VARENICLINE AND SALT THEREOF
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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.
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- Process for Preparing Quinoxaline Derivatives
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The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof.
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Page/Page column 10
(2012/01/14)
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- PROCESS FOR THE PREPARATION OF SUBSTITUTED QUINOXALINES
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The present invention is directed to an improved process for the preparation of substituted quinoxalines by cyclization of the corresponding dianiline in the presence of ion exchange resin.
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Page/Page column 7
(2012/11/08)
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- HIGHLY PURE VARENICLINE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF METHYLVARENICLINE IMPURITY
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Provided herein is an impurity of varenicline, 6-methyl-5,8,14-triazatetracyclo[l 0.3.1.02'n,04'9]hexadeca-2(l l),3,5,7,9-pentaene (methylvarenicline) impurity, and a process for the preparation and isolation thereof. Provided further herein is a highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity, a process for the preparation thereof, and pharmaceutical compositions comprising highly pure varenicline or a pharmaceutically acceptable salt thereof substantially free of methylvarenicline impurity.
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Page/Page column 20
(2011/10/05)
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- IMPROVED PROCESS FOR THE PREPARATION OF SUBSTITUTED QUINOXALINES
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The present invention is directed to an improved process for the preparation of substituted quinoxalines by cyclization of the corresponding dianiline in the presence of ion exchange resin.
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Page/Page column 16-17
(2011/07/30)
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- 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 18
(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 12; 13-14; 17
(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 10
(2009/12/28)
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- PREPARATION OF HIGH PURITY SUBSTITUTED QUINOXALINE
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The present invention comprises an improved process for the preparation of substituted quinoxaline I by cyclization of the corresponding dianiline.
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Page/Page column 8
(2008/06/13)
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- Varenicline: An α4β2 nicotinic receptor partial agonist for smoking cessation
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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.
- 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.
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p. 3474 - 3477
(2007/10/03)
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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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- PREPARATION OF SUBSTITUTED QUINOXALINES FROM THE DIANLINE WITH 2,3-DIHYDROXY-1,4-DIOXANE
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The present invention relates to a new process for the preparation of substituted quinoxalines (I) by cyclization of the corresponding dianiline with 2,3 dihydroxy-1,4-dioxane. In a preferred embodiment, the invention provides a process for the preparation of compounds having the formula III wherein Q is a nitrogen protecting group. Compounds of formula III and their derivatives are precursors to certain aryl fused azapolycyclic compounds which exhibit activity as agents for the treatment of neurological and psychological disorders.
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