| 摘要 |
The invention comprises a process for the preparation of diazines of the formula <FORM:1021195/C2/1> or tautomers thereof, in which Y represents an amino group, R0 represents a hydrocarbon group which may be substituted or a hydrogen atom, and the symbol <FORM:1021195/C2/2> represents an optionally substituted carbocyclic or heterocyclic ring, or of an acid addition salt thereof, by reacting a compound of the formula <FORM:1021195/C2/3> or a tautomer thereof, in which X1 and X2 each represents a free, etherified or esterified hydroxyl group, or together represent an oxo group, with ammonia or an amine of the formula HY, and simultaneously or subsequently treating the resulting compound with a dehydrogenating agent, and, if desired, converting a resulting acid addition salt into a free base or a resulting base into an acid addition salt. The diazines of the formula <FORM:1021195/C2/4> and the 7,8-dihydro derivatives thereof, in which R3 represents a hydrogen atom or a C1- 7 alkyl, di-C1- 7 alkyl-amino, piperidino, pyrrolidino, morpholino or piperazino group and Y represents a di-C1- 7 alkylamino, piperidino, morpholino, pyrrolidino or piperazino group, are claimed per se. Pharmaceutical preparations, having diuretic and sodium-excretive activity, for enteral or parenteral administration, comprise a compound of the Formula IV, or a 7,8-dihydro derivative thereof, together with a pharmaceutical carrier. The preparations may be in the form of tablets, dragees, capsules, solutions, suspensions or emulsions, or in the form of animal feedstuffs or as additives to feedstuffs. |
