| 摘要 |
<p>. The compound Ia Ia (4,5,6,7-tetrahydroisoxazolo5,4-c!pyridine-3-ol) has been shown to possess GABA-related activity. The invention relates to Ia and derivatives thereof, covered by the formula I VII in which R" is hydrogen, acetyl or a group of the general formula VII VII in which R5 is C1-8 alkyl; phenyl; phenyl substituted in the 4-position with halogen, lower alkoxy, or lower alkyl; or phenylalkyl in which the phenyl group may be substituted in the 4-posi-tion with halogen, lower alkoxy, or lower alkyl; and salts thereof. Novel intermediates for preparing I are - la IV in which Alk is a lower alkyl group and Z is hydrogen or an amino-protecting group; VIII' wherein Z is hydrogen or an amino-protecting group, T is a group convertible, by hydrolysis, into an oxy group, and Q is a leaving group which, on reaction with hydroxylamine, forms a hydroxamic acid group; IX' wherein Z and T are as defined above; V wherein Z is as defined above, and W is hydrogen or a group removable to yield the free hydroxy group, with the proviso that at least one of Z and W is different from hydrogen.</p> |
