Intermediates for preparing substituted 1-piperazine-...

C - Chemistry – Metallurgy – 07 – D

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C07D 241/04 (2006.01) C07D 211/46 (2006.01) C07D 295/20 (2006.01) C07D 295/205 (2006.01) C07D 403/06 (2006.01) A61K 31/495 (2006.01) C07D 295/00 (2006.01)

Patent

CA 1237128

ABSTRACT Intermediates which are 1-piperazinecarboxylates or the general formula I Image (I) wherein R2, R3, R4, R5 are groups independently selected from hydrogen, lower alkyl having from 1 to 3 carbon atoms and phenyl, R6 is a group selected from hydrogen, F, C1, Br, lower alkoxy having from 1 to 3 carbon atoms and -CF3- -groups, R1 represents either an unsubstituted or substitu- ted aryl group with good leaving group properties, suitably a phenyl or a para-nitro-phenyl group-, for producing 1-piperazinecarboxamides of the general formula II Image (II) wherein R7 and R8 are groups independently selected from the group of hydrogen, alkyl straight or branched chains having from 1 to 10 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, aralkyl having from 7 to 9 carbon atoms, alkenyl having from 3 to 10 carbon atoms or R7 and R8 represents together with the adjacent nitrogen atom a 4-7 membered ring such as Image wherein m = 0, 1, 2, 3, n = 1 or 2, and Ra is a group selected from lower alkyl having from 1 to 3 carbon atoms, hydroxy-loweralkyl having from 2 to 4 carbon atoms and a lower alkanoyl having from 1 to 3 carbon atoms, A process for preparing the carboxamides of formula II by reacting the 1-piperazinecarboxylates of formula I with an amine of formula III Image (III) wherein R7 and R8 are as defined above, is also described.

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