Process for the preparation of 4-oxoimidazolinium salts

C - Chemistry – Metallurgy – 07 – D

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C07D 235/02 (2006.01) C07D 233/70 (2006.01) C07D 405/02 (2006.01) C07D 409/02 (2006.01)

Patent

CA 2196263

4-Oxoimidazolinium salts of the general formula: (see formula I) wherein R1 and R2 independently of one another are each C1-10- alkyl, C2-10-alkenyl, C3-7 cycloalkyl or optionally substituted aryl, arylalkyl, heteroaryl or heteroarylalkyl, or R1 and R2, together with the carbon atom to which they are bonded, form a three-membered to seven-membered saturated or unsaturated carbocyclic or heterocyclic ring, R3 is a C1-10 alkyl group, C2- 10-alkenyl group, C3-7 cycloalkyl group, aryl group, arylalkyl group or heteroaryl group and A- is an anion of a strong acid, are prepared by the cyclization of an .alpha.-acylaminonitrile in a non-aqueous solvent, in the presence of a lower alcohol and a strong acid. The compounds are intermediates for pharmaceutical active substances, for example angiotensin II antagonists.

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