Studies on psychotropic agents. I. Synthesis of 3,8-disubstituted-1-oxa-3,8-diazaspiro(4,5)decan-2,4-dione derivatives.

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Abstract
A series of 3,8-disubstituted-1-oxa-3,8-diazaspiro[4,5]decan-2,4-diones (XI) were synthesized for pharmacological testing. 3-Substituted-8-benzyl compounds (III), the intermediates of XI, were prepared by the following 3 methods: condensation of methyl 1-benzyl-4-hydroxyisonipecotate (II) with urea, followed by alkylation, treatment of II with isocyanates and reaction of 1-benzyl-4-cyano-4-piperidinol with isocyanates followed by hydrolysis. The last method was inferior to the other 2 methods. Reductive debenzylation of III followed by condensation with appropriate halides afforded XI. The 8-[3-(2-Chlorophenothiazin-10-yl)propyl]3-methyl derivative had excellent CNS depressing activities [mouse, rat].

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