Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof

A process for the preparation of an N-phenyl-2-pyrimidineamine derivative of formula I ##STR10## wherein R.sub.1 is a substituted cyclic radical, the cyclic radical being bonded at a ring carbon atom in each case and being selected from pyridyl, pyrazinyl, thiazolyl, pyrimidinyl, pyridazinyl and imidazolyl, and the substituents of the above-mentioned cyclic radical being selected from one or more of the groups halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.3, --C(.dbd.O)--R.sub.4, --SO.sub.2 --N(R.sub.5)--R.sub.6, --N(R.sub.7)--R.sub.8, --OR.sub.9 and fluorine-substituted lower alkyl, wherein

• R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino;
• and
• R.sub.2 is selected from halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.10, --C(.dbd.O)--R.sub.11, --SO.sub.2 --N(R.sub.12)--R.sub.13, --N(R.sub.14)--R.sub.15, --OR.sub.16 and fluorine-substituted lower alkyl, wherein
• R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15 and R.sub.16 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino, or of a salt of such a compound having at least one salt-forming group, wherein a compound of formula II
• R.sub.1 --C(.dbd.O)--CH.dbd.CH--N(R.sub.17)--R.sub.18 (II),
• wherein R.sub.17 and R.sub.18 are each independently of the other lower alkyl and R.sub.1 is as defined above, functional groups present in a compound of formula II, with the exception of the groups participating in the reaction, being, if necessary, in protected form, or a salt of such a compound is reacted with a compound of formula III ##STR11## wherein R.sub.2 is as defined above, functional groups present in a compound of formula III, with the exception of the guanidino group participating in the reaction, being, if necessary, in protected form, or with a salt of such a compound, and any protecting groups present are removed
• and, if desired, a compound of formula I obtainable in accordance with the above process is converted into its salt, or an obtainable salt of a compound of formula I is converted into the free compound.