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Synthesis and Anticoagulant Activity of New Ethylidene and Spiro Derivatives of Pyrrolo[3,2,1- ij ]quinolin-2-ones
Russian Journal of Organic Chemistry ( IF 0.8 ) Pub Date : 2020-10-19 , DOI: 10.1134/s1070428020090080
N. P. Novichikhina , A. A. Skoptsova , A. S. Shestakov , A. Yu. Potapov , E. A. Kosheleva , O. A. Kozaderov , I. V. Ledenyova , N. A. Podoplelova , M. A. Panteleev , Kh. S. Shikhaliev

Abstract

The reaction of pyrrolo[3,2,1-ij]quinoline-1,2-diones with methyl (het)aryl ketones gave the corresponding 1-(het)arylmethylidenepyrroloquinolin-2-ones, and 1,3-dipolar cycloaddition of the latter to azomethine ylide generated from sarcosine and paraformaldehyde afforded 4-acyl-1,4′,4′,6′-tetramethylspiro[pyrrolidine-3,1′-pyrrolo[3,2,1-ij]quinolin]-2′(4′H)-ones. The synthesized compounds were evaluated for inhibitory activity against blood coagulation factors Xa and XIa.



中文翻译:

吡咯并[3,2,1-ij]喹啉-2-酮的新亚乙基和螺衍生物的合成及抗凝血活性

摘要

吡咯并[3,2,1- ij ]喹啉-1,2-二酮与甲基(杂)芳基酮反应,得到相应的1-(杂)芳基亚甲基吡咯并喹啉-2-酮,且1,3-偶极环加成后者与由肌氨酸和多聚甲醛产生的甲亚胺叶立德反应得到4-酰基-1,4',4',6'-四甲基螺[吡咯烷-3,1'-吡咯并[3,2,1- ij ]喹啉] -2'( 4′H)-个。评价合成的化合物对凝血因子Xa和XIa的抑制活性。

更新日期:2020-10-19
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