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