| 摘要 |
Compounds having the formula <IMAGE> wherein <IMAGE> <IMAGE> R1 is hydrogen, benzyl or an ester moiety; Y is -CH(R2'')CH(R2)- or -CH(R3)CH hd 2-; R2'' is hydrogen or methyl; R2 is OH or X-substituted (C1-6)alkyl; R3 is OH, cyano or X-substituted (C1-3)alkyl; X is -OR6, -SR6, -S(O)R6, -S(O)2R6, -NR6R7, -COOR7, -CONR7R8 or oxo; with the proviso that when X is -NR6R7, -COOR7 or -CONR7R8, said group is located on the terminal carbon atom of R2 or R3; R6 is hydrogen, (C1-6)alkyl or acetyl; each of R7 and R8 is hydrogen or (C1-6)alkyl; s is an integer of 1 or 2; with the proviso that when R6 is acetyl, R7 is hydrogen and X is other than S(O)R6 or S(O)2R6; Z-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain, and their use as CNS agents, antidiarrheals and anti-emetics. Processes for their preparation and intermediates therefor are described.
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