GB1261939A - Tetrahydropyrimidines and process for preparing them - Google Patents

Abstract

1,261,939. Tetrahydropyrimidines. FARBWERKE HOECHST A.G. 11 April, 1969 [13 April, 1968], No. 18650/69. Heading C2C. Novel compounds I (including salts thereof) wherein the groups R<SP>1</SP> may be the same or different and signify 2,4- or 3,4-dichlorobenzyl and R<SP>2</SP> signifies pyridyl or phenyl which carries in the 2- or 4-position NO 2 , CN, SO 2 NH 2 or carbamoyl and which may contain one or more further substituents (halogen, Me and alkoxy) and which carbamoyl may be alkyl substituted or may be disubstituted by C 4-6 alkylene thus forming with the N-atom a heterocyclic ring, are obtained: (a) by reacting a diamine, (R<SP>1</SP>) 2 .C(CH 2 NH 2 ) 2 , with an acid, R<SP>2</SP>.CO 2 H, or with an appropriate derivative thereof; (b) by cyclizing an amide, which is itself obtained by acylation; (c) by reacting a dihalide, (R<SP>1</SP>) 2 .C.(CH 2 X) 2 (X is Cl or Br), with an amidine, R<SP>2</SP>.C(:NH)(.NH 2 ); or (d) by converting a carboxy compound VII (R<SP>3</SP> signifies 2- or 4-carboxy-phenyl optionally substituted by halogen, Me and/or alkoxy) into the corresponding carbamoyl or cyano compound or by diazotizing an amino compound VII (R 3 signifies 2- or 4-amino-phenyl optionally substituted by halogen, Me and alkoxy) and subsequently introducing CN, NO 2 or SO 2 NH 2 . Pharmaceutical preparations suitable for the treatment of protozoal infections contain I as active ingredient; administration may be orally or parenterally.