Process for the preparation of 1-methylamino-...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/10 (2006.01) C07D 215/58 (2006.01) C07F 5/02 (2006.01)

Patent

CA 1294621

A B S T R A C T The present invention relates to a process for the preparation of compounds of the general Formula I Image /I/ and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II Image /II/ (wherein R1 and R2 stand for halogen; an aliphatic acyl- oxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms) with a piperazine of the general Formula III Image /III/ (wherein R3 represents hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general for- mula IV /IV/ Image thus obtained (wherein R, R1 and R2 are as stated above) without or after hydrolysis and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt. The compounds of the general Formula I are known antibacterial agents. The advantage of the process of the present inven- tion is that it enables the preparation of the compounds of the general formula I in a simple manner, with high yields and in a short reaction time.

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