PROCESS FOR THE PREPARATION OF GUANDINO DERIVATIVES OF POLYALKYLENE POLYAMINES

摘要

Novel guanidines of the formula wherein each of R1 and R2 is a hydrogen atom or an alkyl group, each of R6, R7 and R8 is an alkylene group separating adjacent nitrogen atoms by a chain of at least two carbon atoms, the total number of carbon atoms in the straight chain between the groups G1 and G2, excluding branching groups, being always greater than 12, n is 0 to 4 and each of G1 and G2 is a group of the formula wherein each of R3, R4 and R5 is a hydroge atom or a C1- 4 alkyl group, and their physiologicall acceptable acid addition salts, are prepared by (a) reacting a polyamine of the formula with a thiourea of formula in which R9 is an alkyl or aralkyl group, or an acid addition salt thereof, or with cyanamide, or with N-nitrosoguanidine or an N-alkyl-N-nitrosoguanidine, or with a cyanogen halide followed by reaction with ammonia or an amine, or (b) reacting a substituted thiourea of formula with mercuric oxide and ammonia or an amine. The resulting compounds may, if necessary, be alkylated to introduce the alkyl substituents R3, R4 and R5, or converted into the free bases or acid addition salts. Polyamines of Formula III are prepared by reducing the corresponding nitriles, or by condensing alkylene diamines or polyalkylene polyamines with alkylene dihalides.ALSO:Pharmaceutical, horticultural and agricultural compositions having antifungal, anti-bacterial, antiviral, analgesic and antiheparin activity, comprise a compound of the formula: wherein each of R1 and R2 is a hydrogen atom or an alkyl group, each of R6, R7 and R8 is an alkylene group separating adjacent nitrogen atoms by a chain of at least two carbon atoms, the total number of carbon atoms in the straight chain between the groups G1 and G2, excluding branching groups, being always greater than 12, n is 0 to 4 and each of G1 and G2 is a group of the formula: wherein each of R3, R4 and R5 is a hydrogen atom or a C1-4 alkyl group, or a salt thereof, together with a carrier. The pharmaceutical compositions may be in a form suitable for oral, topical, rectal, intravaginal or parenteral administration, e.g. in the form of tablets capsules, solutions, syrups, elixirs, emulsions, sprays, powder insufflations, nasal drops, throat paints, skin paints, lotions, creams ointments, aerosols, dusting powders, suppositories, pessaries or injectable preparations. The horticultural and agricultural compositions may be in the form of solutions, emulsions, dusts, wettable powders, granulates, pellets and pastes.