It is an object of the present invention to provide 2-iminocarboxylic acid derivatives, and a practically suitable industrial method for producing benzazepinones in a short process under mild conditions. The present invention provides a method for producing a benzazepinone or a salt thereof, which comprises opening a ring of an isoquinoline derivative and subsequently converting the thus generated amine into a benzazepinone through lactamization reaction.
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Page/Page column 18
(2008/12/04)
Classical and dynamic resolution of 1-amino-3-methyl-1,3,4,5- tetrahydrobenzo[d]azepin-2-one
Two efficient production processes of enantioenriched 1-amino-3-methyl-1,3, 4,5-tetrahydro-benzo[d]azepin-2-one 1 were achieved using the readily available starting materials. A key step in the methodologies is a classical resolution or a dynamic resolution that provides excellent chemical (>80%) yields and enantiomeric excesses (>99.8% ee). The classical resolution was developed on a preparative scale while the dynamic resolution was implemented on a pilot plant scale.
Mitchell, David,Hay, Lynne A.,Koenig, Thomas M.,McDaniel, Stacey,Nissen, Jeffrey S.,Audia, James E.
p. 3814 - 3819
(2007/10/03)
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