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On the relocation of the amino functionality to the ethyl side chain in aminoglutethimide: Synthesis and aromatase-inhibitory activity of 3-(2′-N,N-diethyl-amino)ethyl-3-phenylpiperidine-2,6-dione by George A. Moniz; Gerald B. Hammond is a Chemistry article available to read on EtoBox.

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## Abstract Aminoglutethimide [3‐(4‐aminophenyl)‐3‐ethylpiperidine‐2,6‐dione] has been used clinically in the treatment of metastatic breast carcinoma. Inhibition of tumor growth is due to interference with estrogen biosynthesis. However, its action is not specific and its metabolism gives rise to toxic and non‐inhibitory metabolites. We sought to explore the impact of relocating the amino group in aminoglutethimide to the ethyl side chain. To that end, we now report the synthesis and aromatase‐inhibitory activity of 3‐(2′‐__N,N__‐diethylamino)ethyl‐3‐phenylpiperidine‐2,6‐dione 5. The introduction of the amino functionality on the ethyl group is accomplished __via__ reductive animation of aldehyde 8, prepared in three steps from benzyl cyanide. The synthetic route presented can be used for the preparation of related derivatives of aminoglutethimide.

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Author

George A. Moniz; Gerald B. Hammond

Publisher

Journal of Heterocyclic Chemistry; Wiley (John Wiley & Sons); Wiley-Blackwell; Wiley; FASEB (ISSN 0022-152X)

Published

1997

Language

EN

Field

Chemistry (Physical Sciences)