Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines as potential central nervous system agents. 2. Compounds containing a heteroatom attached to nitrogen

Journal of Medicinal Chemistry
1977.0

Abstract

The synthesis and antitetrabenazine activity of a series of N-heteroatom derivatives of 3-phenylspiro[isobenzofuran-1,4'-piperidines] are reported. Optimal antitetrabenazine activity is associated with compounds containing a sterically unhindered, basic nitrogen. Hydroxylamines 6, 11, 12, and 13 possess the most significant activity with ED50's of 1.4, 3.5, 4.7, and 4.0, respectively.

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