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Updated: Mar 26, 2026

Optimization of the Ugi Reaction Using Parallel Synthesis and Automated Liquid Handling
Published on: November 11, 2008
Versatile Protecting-Group Free Tetrazolomethane Amine Synthesis by Ugi Reaction
Pravin Patil1, Michel de Haan1, Katarzyna Kurpiewska2
1University of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Abstract:
The use of ammonia in the Ugi reaction is often problematic due to low yields and multiple side reactions. Here, we report the use of ammonia in the tetrazole Ugi variation providing a clean, good-to-high yielding reaction, especially with ketones as oxo components. The scope and limitations of this reaction and a structure-reactivity relationship are provided by performing >85 reactions. The primary amine component of the α-amino tetrazole is a versatile starting material for further reactions.
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