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A convenient solution and solid-phase synthesis of Δ5-2-oxopiperazines via N-acyliminium ions cyclization

✍ Scribed by Jie-Fei Cheng; Mi Chen; Thomas Arrhenius; Alex Nadzan

Publisher: Elsevier Science
Year: 2002
Tongue: French
Weight: 95 KB
Volume: 43
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(02)01403-x

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✦ Synopsis

An extremely efficient synthesis of D 5 -2-oxopiperazines in solution phase and on solid support has been established via a Ugi four-component condensation reaction (U-4CC) followed by N-acyliminium ion cyclization between the aldehyde (acetal) functionality and the newly formed amide bond. The desired D 5 -2-oxopiperazines are obtained in excellent yields and purity.

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