Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226031, Uttar Pradesh, India.
Chemical Sciences Division, Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, Uttar Pradesh, India.
J Org Chem. 2020 Dec 4;85(23):14890-14904. doi: 10.1021/acs.joc.0c01539. Epub 2020 Nov 2.
An efficient method for the generation of uniquely functionalized pyrrolo-pyrrolizinones, pyrido-pyrrolizinones, and azepino-pyrrolizinones via [3 + 2]-dipolar cycloaddition is described. The method involves the synthesis of tethered alkynamides using Ugi condensation and oxidation that were subsequently subjected to a dipolar cycloaddition reaction with trimethylsilyl amino esters. Further transformations to demonstrate the utility of these scaffolds were also investigated.
描述了一种通过[3+2]-偶极环加成高效合成独特官能化吡咯并吡咯里嗪酮、吡啶并吡咯里嗪酮和氮杂并吡咯里嗪酮的方法。该方法涉及使用 Ugi 缩合和氧化合成连接的炔酰胺，然后与三甲基硅基氨基酯进行偶极环加成反应。还研究了进一步的转化以证明这些支架的实用性。
