Processes for preparing aminophenylsulfonylureas, and...

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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Reexamination Certificate

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07057043

ABSTRACT:
The invention relates to the preparation of compounds (I)in which A=H or acyl and R1, R2, R3, R, n, X, Y and Z are as defined in claim1by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III)in-line-formulae description="In-line Formulae" end="lead"?R*═OH, R**═NR1R2  (II)in-line-formulae description="In-line Formulae" end="tail"?in-line-formulae description="In-line Formulae" end="lead"?R*═NR1R2, R**═Cl  (III)in-line-formulae description="In-line Formulae" end="tail"?in-line-formulae description="In-line Formulae" end="lead"?R*═NR1R2, R**═NH2  (IV)in-line-formulae description="In-line Formulae" end="tail"?a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)-Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), orb) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2group to give compounds (I) (A=H), orc) reaction of (III) with cyanates and amines (V) of the formula HNR3−Het and reduction of the resulting compound (VII) at the NO2group to give compounds (I) (A=H) and optional acylation if A is to be other than H. Compounds of the formulae (I) (A=H), (III), (IV), (V), (VI) (M=cation) and (VII) are novel.

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