Abstract: A process for the production of 2,4-diamino-5-(3',4',5'-trimethoxybenzyl)-pyrimidine by condensing trimethoxy benzaldehyde with a substituted propionitrile compound and reacting the condensation product obtained with guanidine, wherein a .beta.-akyl-(aryl-, benzyl-)-oxy-ethyleneoxy-propionitrile corresponding to the formulaR--O--CH.sub.2 --CH.sub.2 --O--CH.sub.2 --CH.sub.2 --CN (I)in which R represents an alkyl group, an optionally substituted phenyl group or a benzyl group, is condensed with trimethoxy benzaldehyde in the presence ofBasic reagents to form a compound corresponding to the general formula ##STR1## in which R is as defined above, and the condensation product (II) obtained is reacted with guanidine in known manner to form 2,4-diamino-5-(3',4',5'-trimethoxybenzyl)-pyrimidine.
Abstract: This invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 independently represent groups selected from the group consisting of straight chain alkyl groups; branched chain alkyl groups; aryl groups; optionally substituted aryl groups and the groups required to complete a ring system together with the sulphur atom;R.sup.3 and R.sup.4 independently represent groups selected from the group consisting of hydrogen; straight chain alkyl groups; branched chain alkyl groups and optionally substituted aryl groups;R.sup.5 and R.sup.6 independently represent groups selected from the group consisting of alkyl groups and the groups required to complete a heterocyclic ring together with the nitrogen atom; the groupR.sup.7 represents a group selected from the group consisting of hydrogen; straight chain alkyl groups and branched chain alkyl groups;X represents an anion of a physiologically acceptable acid andn represents a number selected from the group consisting of 0 and 1.
Type:
Grant
Filed:
September 2, 1976
Date of Patent:
August 8, 1978
Assignee:
Ludwig Heumann & Co. GmbH.
Inventors:
Manfred Haake, Reinhold Pothmann, Kurt H. Ahrens, Edgar Fritschi
Abstract: Bactericidal 4'-alkyldioxyalkylene-5-benzylpyrimidines, process for their production, and pharmaceutical compositions or formulations thereof, containing compounds of the general formula: ##SPC1##Wherein R.sub.1 is an alkyl group containing from 1 to 3 carbon atoms, R is an atom of hydrogen, an atom of halogen, or an alkyl or alkoxy group containing from 1 to 3 carbon atoms, and n is an integer of from 1 to 3,Exhibit excellent bactericidal activity and low toxicity and are suitable for oral administration.