230615-48-2Relevant articles and documents
Synthesis of 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepine via oxidative cleavage and reductive amination strategies
Brooks, Paige R.,Caron, Stephane,Coe, Jotham W.,Ng, Karl K.,Singer, Robert A.,Vazquez, Enrique,Vetelino, Michael G.,Watson Jr., Harry H.,Whritenour, David C.,Wirtz, Michael C.
, p. 1755 - 1758 (2004)
Preparations of 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepine (5) from benzonorbornadiene (1) by oxidative cleavage and reductive amination sequences were investigated. Osmium-mediated dihydroxylation of 1 followed by NaIO 4 cleavage, reductive amination and debenzylation provides 5 in 64-73% yield overall in three operations. A tandem ozonolysis-reductive amination procedure gives 5 as the tosylate salt from benzonorbornadiene with no isolation of intermediates in 28% yield.
Process for preparing varenicline and intermediates for use therein
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Page/Page column 10, (2010/07/10)
The present invention relates to an improved process for preparing varenicline, or pharmaceutically acceptable salts or solvates thereof, and in particular an improved process for preparing varenicline, or pharmaceutically acceptable salts or solvates thereof, employing intermediate compounds 1,2,3,4-tetrahydro-1,4-methano-naphthalene-cis-2,3-diol (a compound of Formula III), and / or indane-1,3-dicarbaldehyde (a compound of Formula IV) as prepared by a process of the present invention.
Aryl fused azapolycyclic compounds
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, (2008/06/13)
Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; a