4.0 Article

Synthesis and Anticoagulant Activity of New Functionalized 4H-Pyrrolo[3,2,1-ij]quinolin-2-ones

期刊

RUSSIAN JOURNAL OF ORGANIC CHEMISTRY
卷 58, 期 9, 页码 1225-1232

出版社

MAIK NAUKA/INTERPERIODICA/SPRINGER
DOI: 10.1134/S1070428022090056

关键词

4H-pyrrolo[3; 2; 1-ij]quinolin-2-one; Wolff-Kishner reaction; anticoagulant activity; factors Xa and XIa

资金

  1. Russian Science Foundation [18-74-10097]

向作者/读者索取更多资源

In this study, new compounds with different skeletal structures were synthesized through selective reduction reactions and their anticoagulant activity was evaluated.
The reduction of 4,4,6-trimethyl-4H-pyrrolo[3,2,1-ij]quinoline-1,2-diones with aqueous hydrazine hydrate selectively involved the C-1=O carbonyl group to give the corresponding 4,4,6-trimethyl-4H-pyrrolo-[3,2,1-ij]quinolin-2(1H)-ones within a few hours. The reduction products were condensed with aldehydes and acetone to afford new 1-[(het)arylmethylidene]- and 1-(propan-2-ylidene)-4H-pyrrolo[3,2,1-ij]quinolin-2(1H)-ones in 59-78% yield. The reaction of 4,4,6-trimethyl-4H-pyrrolo[3,2,1-ij]quinolin-2(1H)-ones with N,N-di-methylformamide dimethyl acetal, followed by transamination with primary amines led to the formation of 1-{[(het)arylamino]methylidene}-4H-pyrrolo[3,2,1-ij]quinolin-2-ones in 65-83% yield. The synthesized compounds were evaluated for their anticoagulant activity by measuring inhibition of blood coagulation factors Xa and XIa.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.0
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据