ACS Comb Sci. 2012 Mar 12;14(3):160-3. doi: 10.1021/co200209a. Epub 2012 Feb 15.
A one-pot, two-step synthesis of bis-pyrrolidinone tetrazoles has been established via the Ugi-Azide reaction using methyl levulinate, primary amines, isocyanides and azidotrimethylsilane with subsequent acid treatment to catalyze the lactam formation. The efficiency of the protocol was established followed by a successful transition to library production in four 24-well plates.
建立了一种通过 Ugi-Azide 反应一锅两步合成双吡咯烷酮四唑的方法,使用甲基戊二酸酯、伯胺、异氰化物和叠氮三甲基硅烷,随后进行酸处理以催化内酰胺形成。该方案的效率得到了确立,随后成功地在四个 24 孔板中进行了文库生产的转化。