Process for the preparation of new 2-(2-thienyl)-...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01)

Patent

CA 1297107

Abstract The invention relates to a process for the pre- paration of new 2-(2-thienyl)imidazo(4,5-c)pyridine derivatives of the general formula Image wherein R1 denotes lower alkyl, R2 denotes hydrogen or methyl and n denotes 0 or 1, and pharmaceutically usable acid addition salts thereof, by reacting a thiophenecar- boxylic acid chloride of the general formula III with a diaminopyridine of the general formula IV of the descrip- tion to give an isomer mixture consisting of amides of the general formula Image V, wherein R1 and R2 are as defined in formula I, one of the symbols A and B denotes the =N atom and the other in each case denotes =CH-, then cyclizing the isomer mixture in the form of the hydrochlorides and, if appropriate, oxidizing a resulting compound of the formula I in which n denotes 0 to give a compound of the formula I in which n denotes 1 by treatment with organic peracids or hydrogen peroxide, and, if desired, converting the resulting com- pounds of the formula I into pharmaceutically usable salts. The new compounds have useful pharmacological proper- ties, in particular a strongly positively inotropic action, and can be used as active compounds for medicaments for the treatment of diseases of the heart and vessels, in particular myocardial insufficiency.

519580

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