| 摘要 |
This invention relates to a process for preparing derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one of general formula (I) <IMAGE> (I) in which R is hydrogen, halogen or methyl; R1 and R2 are linear or branched C2-C4 alkyl groups, which alternatively may be joined together to give a piperazine cycle which can be substituted in position 4 with a methyl, ethyl or benzyl group, and their salts with organic and inorganic acids, characterised by comprising the following stages: (a) reacting a compound of general formula (X), <IMAGE> (X) in which R has the meaning heretofore defined, with 2-cloro-3-amino-pyridine of formula (III) <IMAGE> (III) in the presence of polyphosphoric acid, to give an intermediate of general formula (II) <IMAGE> (II) (b) reacting said intermediate with a compound of general formula (XI) <IMAGE> (XI) in which R1 and R2 have the meaning heretofore defined and R3 is a hydroxyl or halogen, in an inert solvent at a maximum temperature equal to the solvent boiling point, to give said derivatives of general formula (I). The invention also relates to the final compounds thus obtained, and the synthesis intermediates obtained during the course of said process. The final products of formula (I) are of great interest in the pharmaceutical field.
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