| 摘要 |
Compounds where R1 = substituted amino, or heterocyclic group, i.e. where R3 and R4 are H, alkyl, alkenyl, aralkyl or cycloalkyl, but both R3 and R4 cannot be H; or R1 = heterocyclic which may be aziridinyl, azetidinyl, pyrrolidinyl, piperidino, hexahydroazepinyl, heptamethyleneimino, acetamethyleneimino, morpholino, or 4-lower alkyl-piperazinyl. The heterocyclic group may also be substituted on a C atom with 0 to 3 lower alkyl and is attached to the pyrimidine (I) via the N-atom. and R = H, alkyl, alkenyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, alkaryl, alkaralkyl, alkoxyaralkyl, lower halogenaralkyl, chloro, bromo, iodo, nitroso, nitro, amino, phenylthio, lower alkylphenylthio, halogenphenylthio, and any of the values of R1. The silicofluorides of (I) are moth-preventing, the thiocyanates form resins with formaldehyde which are corrosion inhibitors, the compounds (I) also form salts with penicillin which are used for the separation and purification of penicillins, especially benzyl penicillin. In addition, the compounds (I) and the acid addition salts and the carboxyacylates are orally and parenterally acting antihypertensives, blood-pressure lowering agents, anti-fertility agents, antiseptics, and are useful for the treatment of shock. 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine, m.p. 262-264 deg.C. |
