Tricyclische Verbindungen

摘要

The invention relates to D-(-)a -aminobenzylpenicillin trihydrate. This compound is prepared by contacting an acid addition salt of D-(-)-a -aminopenicillin with an amine of general formula wherein R is an aliphatic group having 10 to 15 carbon atoms, R1 is hydrogen or C1-C6 alkyl and R2, R3 and R4 are each alkyl and wherein R2, R3 and R4 contain in aggregate from 11 to 14 carbon atoms, in a water-immiscible organic solvent containing at least 3 moles of water per mole of D-(-)-a aminobenzylpenicillin at a temperature below 60 DEG C. and recovering the precipitate of D-(-)-a -aminopenicillin trihydrate. The acid addition salt may be with inorganic or organic acids especially aryl sulphonic acids of formula R5SO3H wherein R5 is or in which R6, R7, R8 and R9 are hydrogen, C1-C12 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, nitro, C1-C6 alkanoylamino, C1-C6 alkanoyloxy, sulphanyl, chloro, iodo, bromo, fluoro, trifluoromethyl, C1-C6 alkylsulphonyl, benzyl, carbo C1-C6 alkoxy, phenethyl, cycloheptyl, cyclohexyl, and cyclopentyl, especially the p-nonylbenzene sulphonate and p-toluene sulphonate or the p-cymene sulphonate. The preferred water-immiscible solvent is methylisobutylketone. The penicillin is insoluble in water, stable on storage, resistant to destruction by acids and is a potent antibacterial agent for pharmaceutical and veterinary use, e.g. treating mastitis in cattle. It may be incorporated into animal feeds or formulated into pharmaceutical compositions. Specification 873,049 is referred to.