Imidazolylphenyl amidines, processes for their preparation...

C - Chemistry – Metallurgy – 07 – D

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C07D 233/64 (2006.01)

Patent

CA 1181080

ABSTRACT OF THE DISCLOSURE The invention relates to a process for preparing a compound of formula IX Image (IX) in which R and R1, which may be the same or different, each represents a hydrogen atom or a lower alkyl group, and B represents a cyano, acetyl, carbethoxy or carbamyl group, or an acid addition salt thereof, which process comprises reacting an amine of formula II Image (II) (wherein R is as defined above) with a compound of formula X Image (X) wherein R1 and B are as defined above, or in the case where B represents a cyano group, reacting an amine of formula II with cyanamide in the presence of a compound of formula VII Image (VII) where R1 is as defined above and Y is a lower alkyl group and, where required, forming an acid addition salt thereof. The invention further relates to compounds of formula (IX) as defined above or acid addition salts thereof. Compounds of formula (IX) are useful as intermediates in the preparation of pharmacologically active substituted imidazolylphenyl amidines which are H2 receptor blocking agents inhibiting gastric acid secretion (as antiulcer agents).

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