| 摘要 |
A process for the preparation of 2 (S),4 (S),5 (S),7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides of formula (I) and their physiologically acceptable salts, and the new compounds used as intermediates in the multistage process is disclosed, wherein the double bond of 2,7dialkyl-8-aryl-4-octenic acid or 2,7-dialkyl-8-aryl-4-octenic acid ester of formula (II) is simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted to a hydroxylactone and then the hydroxy group is converted to a leaving group, the leaving group substituted with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain octanoyl amide compounds of formula (I), and wherein: wherein: R1 and R2 are, independently of one another, H, C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxy, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1-C6alkyloxy; R3 is C1-C6alkyl; R4 is C1-C6alkyl; and R5 is C1-C6alkyl, C1-C6hydroxyalkyl, C1-C6alkoxy-C1-C6-alkyl, C1-C6alkanoyloxy-C1-C6alkyl, C1-C6aminoalkyl, C1-C6alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6alkanoylamido-C1-C6-alkyl, HO(O)C-C1-C6-alkyl, C1-C6alkyl-O(O)-C-C1-C6alkyl, H2N-C(O)-C1-C6alkyl, C1-C6alkyl-HN-C(O)-C1-C6alkyl or (C1-C6alkyl)2N-C(O)-C1-C6-alkyl. |
