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β-氰乙基异氰酸酯在 Ugi 四唑反应中的可裂解性。

Cleavable β-Cyanoethyl Isocyanide in the Ugi Tetrazole Reaction.

机构信息

University of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.

Jagiellonian University , Department of Crystal Chemistry and Crystal Physics, Ingardena 3, 30-060 Krakow, Poland.

出版信息

Org Lett. 2016 Oct 7;18(19):4762-4765. doi: 10.1021/acs.orglett.6b01826. Epub 2016 Sep 9.

Abstract

β-Cyanoethyl isocyanide is introduced as a cleavable isocyanide in the Ugi tetrazole reaction. Eleven examples are described that exhibit a broad scope and are obtained in good overall yields. The obtained 1H-tetrazole scaffold is an important bioisostere for carboxylic acids, and the method described here is a valuable alternative route to known procedures.

摘要

β-氰乙基异氰酸酯被引入到 Ugi 四唑反应中作为一种可裂解的异氰酸酯。描述了 11 个实例,它们表现出广泛的适用范围,并以良好的总收率得到。所得到的 1H-四唑支架是羧酸的重要生物等排体,这里描述的方法是替代已知方法的有价值的途径。

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