Process for the preparation of pyridinecarboxylic acid...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/02 (2006.01) C07D 213/81 (2006.01) C07D 401/00 (2006.01)

Patent

CA 1103252

ABSTRACT OF THE DISCLOSURE The invention relates to a new process for the preparation of pyridinecarboxylic acid piperazides having the general formula I Image (I) and their acid addition salts. In the general formula I R1 stands for a methyl or a benzyl group. These compounds are prepared by reacting an organic or inorganic salt of pyridinecarboxylic acid with a chloroformic acid ester of the general formula III Image (III) wherein R stands for an alkyl having from 1 to 3 carbon atoms in the presence of an inert solvent, and the compound of the general formula IV Image (IV) obtained, wherein R has the same meaning as defined above, is further reacted with a substituted piperazine of the general formula V Image (V) wherein R1 has the same meaning as defined above, The compounds of the general formula I possess valuable cardiovascular and antidepressant properties and can be obtained by the process according to the invention almost quantitatively, in an excellent purity.

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