Patil Pravin, de Haan Michel, Kurpiewska Katarzyna, Kalinowska-Tłuścik Justyna, Dömling Alexander
University of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Jagiellonian University , Faculty of Chemistry, Department of Crystal Chemistry and Crystal Physics, Biocrystallography Group, Ingardena 3, 30-060 Kraków, Poland.
ACS Comb Sci. 2016 Mar 14;18(3):170-5. doi: 10.1021/acscombsci.5b00189. Epub 2016 Feb 22.
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.
在乌吉反应中使用氨往往存在问题，因为产率低且会发生多种副反应。在此，我们报道了在四氮唑乌吉反应变体中使用氨的情况，该反应提供了一种清洁、产率良好至高的反应，特别是当酮作为羰基组分时。通过进行超过85个反应，给出了该反应的适用范围和局限性以及结构 - 反应性关系。α - 氨基四氮唑的伯胺组分是用于进一步反应的通用起始原料。
