Pharmacologically active 2-hydroxy-4- (substituted)phenyl...

C - Chemistry – Metallurgy – 07 – C

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C07C 39/17 (2006.01) C07C 39/23 (2006.01) C07C 39/42 (2006.01) C07C 45/44 (2006.01) C07C 45/51 (2006.01) C07C 45/59 (2006.01) C07C 45/60 (2006.01) C07C 45/64 (2006.01) C07C 45/67 (2006.01) C07C 45/69 (2006.01) C07C 47/27 (2006.01) C07C 47/277 (2006.01) C07C 47/46 (2006.01) C07C 47/47 (2006.01) C07C 49/245 (2006.01) C07C 49/255 (2006.01) C07C 49/747 (2006.01) C07C 49/753 (2006.01) C07C 49/757 (2006.01) C07C 69/66 (2006.01) C07D 209/48 (2006.01) C07D 303/32 (2006.01)

Patent

CA 1170656

ABSTRACT Compounds having the formula Image (I) wherein R is hydroxy or lower alkanoyloxy; R1 is hydrogen, lower alkanoyl or a hydroxy protecting group; Y is -CH(R2")CH(R2)- or -CH(R3)CH2-; 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, -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 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, antldiarrheals and antiemetics. Processes for their pre- paration and intermediates therefor are described.

386091

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