| 摘要 |
1409768 2 - Guanidinylidene -imidazolidines and hexahydropyrimidines DR KARL THOMAE GmbH 7 Feb 1973 [8 Feb 1972] 6072/73 Heading C2C Novel compounds I in which R 1 and R 2 are hydrogen or C 1-4 alkyl or one of R 1 and R 2 is additionally hydroxyl, R 3 and R 4 are hydrogen or C 1-4 alkyl, R 5 is hydrogen, C 1-6 alkyl, C 2-3 hydroxy alkyl, phenyl (optionally mono- or di-substituted by C 1-2 alkyl, C 1-2 alkoxy, fluorine, chlorine, bromine or cyano), a benzyl or phenethyl group (optionally mono- or di-substituted by halogen atoms or an adamantyl group), R 6 is hydrogen or C 1-4 alkyl, R 7 is hydrogen, C 1-6 alkyl, C 2-3 hydroxyalkyl, a benzyl or phenethyl group (optionally substituted by alkyl or alkoxy groups of 1 to 2 C atoms), phenyl (optionally substituted by chlorine, carboxyl or amino sulphonyl radicals or an adamantyl group) and R 8 is hydrogen or C 1-4 alkyl or NR 7 R 8 represents a 5 to 7 membered saturated heterocyclic ring optionally containing an oxygen or sulphur atom or a further nitrogen atom optionally substituted by C 1-3 alkyl or phenyl and n is 0 or 1 are prepared by reacting a novel cyanimino compound II with an amine HNR 7 R 8 or with its hydrochloride. Compounds I (R 6 =H) are also prepared by reacting an S-alkylthiourea IV in which R 9 is alkyl with the amine HNR 7 R 8 . The imidazolidine derivatives of Formula I may be purified by forming their sparingly soluble crystallizable copper complexes which are dissolved in a dilute mineral acid and the copper removed by precipitation with hydrogen sulphide. Novel compounds II are prepared by reacting an N-cyanimino-dithiocarbonic acid in which R 10 is alkyl or both together represent ethylene, with a compound Novel compounds IV are prepared by reacting 2 - cyanimino - imidazolidines or hexahydropyrimidines with hydrogen sulphide to form compounds VII which are reacted with alkyl iodides. Compounds I have an anti-microbial and virucidal activity and cause a lowering of blood-sugar levels. They form with a carrier or excipient a pharmaceutical composition which may be administered orally or topically. |
