Abstract
Possible analogues of baclofen, 3-aminomethyl-5-chloro-, 3-aminomethyl-6-chloro- and 3-aminomethyl-5, 6-dichloro-isobenzofuran-1(3H)-one, have been prepared for evaluation as antispasticity agents. The corresponding 3-hydroxyisobenzofuran-1(3H)-one was reacted with ethyl acetoacetate under acidic conditions, and the keto ester hydrolysed and decarboxylated to give the 3-(2-oxopropyl)isobenzofuran-1(3H)-one; this was treated with hydrazoic acid, and the productwas hydrolysed. A parallel series of (3-oxo-1, 3-dihydroisobenzofuran-1-yl)glycines was obtained by treating the keto ester first with hydrazoic acid, and hydrolysis of the resulting acetamides.
Original language | English |
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Pages (from-to) | 787-795 |
Number of pages | 9 |
Journal | Australian Journal of Chemistry |
Volume | 42 |
Issue number | 6 |
DOIs | |
Publication status | Published - 1989 |