| 摘要 |
1298525 Butyramidine derivatives ORSYMONDE 27 May 1971 [29 June 1970 1 April 1971] 17558/71 Heading C2C Novel compounds I in which A is α- or #-naphthyl; R 3 is H or 1-3 C alkyl; R 2 is H, OH or 1-3 C alkyl; and R 1 is H; or R 1 and R 2 together with the two N atoms and C atom of the amidine moiety form a 2-imidazolinyl or 1,4,5,6-tetrahydro-2-pyrimidinyl radical when R 3 is H are prepared by con - densing α- or #-naphthol with epichlorohydrin in the presence of caustic soda; treating the 3- naphthyloxy 1,2 - epoxy propane with- HCl gas; reacting the resultant 1-chloro-3-naphthyloxy- 2 -propanol with KCN; reacting the 4- naphthyloxy - 3 - hydroxy - butyronitrile with ethanol to give the imino ether derivative and reacting the latter with an amine HNR 2 R 3 . Compounds I where R 1 =R 2 =R 3 =H may be reacted with NH 2 OH, H 2 NCH 2 CH 2 NH 2 or H 2 N(CH 2 ) 3 NH 2 to transform the amidine function into-C(NH)NHOH, imidazolin-2-yl or tetrahydropyrimidinyl respectively. The preparation of ethyl 4 - α - naphthyloxy- 3 -hydroxy -butyrate from 4-α-naphthyloxy-3-hydroxy-butyroimino-ethyl ether by hydrolysis and its conversion to 4α-naphthyloxy-3-hydroxybutyrohydroxamic acid are described. Pharmaceutical compositions for oral or parenteral administration as agents for treating cardiac troubles comprise a compound I together .with a suitable carrier or excipient. |
