Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

Patent Number: 8110691
Publication Date: 2012-02-07
Inventors: Tuba, Zoltán; Visky, György; Dancsi, Lajosné ; Csörgei, János; Molnár, Csaba; Magyari, Endréné

A new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I)

which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII)

and (VIII)

used as intermediates in the ...

Methods of preparing substituted tetracyclines with transition metal-based chemistries

Patent Number: 8106225
Publication Date: 2012-01-31
Inventors: Koza, Darrell J.; Rennie, Glen; Nelson, Mark L.

The present invention relates to novel chemistries which allow for heretofore unobtainable substituted tetracycline compounds which exhibit significant activity in tetracycline responsive states. The methods disclosed herein utilize reactive tetracycline-based precursor compounds, reactive organic substituent precursors and transition metal catalysts under conditions such that a tetracycline compound substituted with the desired organic substituent is formed. In one embodiment of the ...

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Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

Methods of preparing substituted tetracyclines with transition metal-based chemistries