Resolution process for benzazepine intermediates

C - Chemistry – Metallurgy – 07 – D

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260/241.4

C07D 223/16 (2006.01) C07D 401/12 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2002396

HA476 RESOLUTION PROCESS FOR BENZAZEPINE INTERMEDIATES Abstract In accordance with the present invention an improved process for preparing resolved compounds of the formula I Image being the cis(+) isomer, is disclosed, wherein R1 and R2 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, diarylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, Image , fluoro substituted alkoxy, fluoro substituted alkyl, (cycloalkyl)alkoxy, -NO2, NX3X4 , -S(O)malkyl, -S(O)maryl, Image , or Image ; m is 0, 1 or 2; HA476 X1 and X2 are each independently hydrogen, alkyl, aryl or heteroaryl, or X1 and X2 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl or morpholinyl; X3 and X4 are each independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or Image ; X5 is hydroxy, alkoxy, aryloxy, amino, alkylamino or dialkylamino; and X6 is alkyl, alkoxy or aryloxy; with the proviso that if R4 is a 7-alkyl group, it must have a tertiary carbon atom bonded to the ring.

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