Potential GABAB Receptor Antagonists. III. Folded Baclofen Analogs Based on Phthalide
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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-l(3H)-one was reacted with ethyl acetoacetate under acidic conditions, and the keto ester hydrolysed and decarboxylated to give the 3-(2-oxopropyl)isobenzofuran-l(3H)-one; this was treated with hydrazoic acid, and the product was hydrolysed. A parallel series of (3-oxo-1,3-dihydroisobenzofuran-1-y1)glycines was obtained by treating the keto ester first with hydrazoic acid, and hydrolysis of the resulting acetamides.
1990 ◽
Vol 342
(2)
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pp. 194-197
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1993 ◽
Vol 14
(11)
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pp. 391-394
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1998 ◽
Vol 362
(1)
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pp. 27-34
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2001 ◽
Vol 430
(2-3)
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pp. 251-259
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