| 摘要 |
Process for obtaining piperazinyl carboxamides of general formula I in which Het is a 3-pyridyl or 4-pyridyl radical optionally substituted with a halogen or C1-C4 alkyl thio group in any of the free positions except at the nitrogen, and in any case the pyridine nitrogen can be further substituted by a C1-C4 alkyl group or may be in the form of an N-oxide, Z is a carbonyl, thiocarbonyl, sulphonyl or -CHY- group in which Y is hydrogen, C1-C4 alkyl, carbamoyl or phenylthio, R is a 3,4,5-trimethoxy phenyl, (Ph)2CH-(CH2)g-, (Ph)2(C(OH)-(CH2)g- group in which g is 0, 1 or 2, or (Ph)2CH-NR1-(CH2)p-group in which p is 1 or 2 and R1 is hydrogen or C1-C4 alkyl. According to the process amine II is reacted with HetCOOH through a dehydration process (Z = CO) with HetCHO in the presence of sulphur (Z=CS), with HetSO2Cl (Z = SO2), with HetCHYX (Z=CHY), with HetCHO in the presence of thiophenyl (Z = CH(SPh)-) or with HetCHO in the presence of potassium cyanide, followed by treatment with (Z=CH(CONH2)-) hydrochloric acid. These products are used in the treatment of diseases caused by platelet activating factor (PAF). <IMAGE>
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