One-pot conversion of sustainable D-ribose with L-amino acid, methyl esters produced pyrrole-2-carbaldehydes 5 in reasonable yields (32–63%) under pressurized conditions of 2.5 atm at 80 °C. The value-added pyrraline compounds 5 as platform chemicals were utilized for quick installation of poly-heterocyclic cores for the development of pyrrole-motif natural and artificial therapeutic agents. A pyrrole-fused piperazin-2-one scaffold 6 was prepared by reductive amination of pyrralines 5 with benzylamine. While further cyclization of pyrralines 5 with ethane-1,2-diamine produced pyrrolo-piperazin-2-ones 7 with an extra imidazolidine ring, the reaction with 2-amino alcohols derived from natural L-amino acids, alanine, valine, and phenylalanine, respectively provided pyrrolo-piperazin-2-ones 8, 9, and 10 with oxazolidine as the third structural core. Cell viability and an anti-inflammatory effect of the synthesized compounds were briefly tested by the MTT method and the Griess assay, among which 8h and 10g exhibited significant anti-inflammatory effects with negligible cell toxicity.

中文翻译：

---

核糖与氨基酸转化为吡咯啉平台化学品——多种吡咯融合生物碱化合物的快速合成

可持续D-核糖与L-氨基酸甲酯的一锅转化在 2.5 atm 和 80 °C 的加压条件下以合理的产率 (32–63%)产生 pyrrole-2-carbaldehydes 5 。作为平台化学品的增值吡咯啉化合物5被用于快速安装多杂环核心，以开发吡咯基序的天然和人工治疗剂。通过吡咯啉5与苄胺的还原胺化制备吡咯稠合的哌嗪-2-酮支架6 。而吡咯啉5与 ethane-1,2-diamine 的进一步环化产生 pyrrolo -piperazin-2-ones 7具有额外的咪唑烷环，与衍生自天然L-氨基酸、丙氨酸、缬氨酸和苯丙氨酸的 2-氨基醇反应，分别提供 pyrrolo-pirazin-2-ones 8、9和10，其中恶唑烷作为第三个结构核心. 通过MTT法和Griess法对合成的化合物的细胞活力和抗炎作用进行了简要测试，其中8h和10g表现出显着的抗炎作用，细胞毒性可忽略不计。