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Novel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature
Beilstein Journal of Organic Chemistry ( IF 2.7 ) Pub Date : 2021-01-18 , DOI: 10.3762/bjoc.17.16
Romain Pierre , Anne Brethon , Sylvain A Jacques , Aurélie Blond , Sandrine Chambon , Sandrine Talano , Catherine Raffin , Branislav Musicki , Claire Bouix-Peter , Loic Tomas , Gilles Ouvry , Rémy Morgentin , Laurent F Hennequin , Craig S Harris

In our hands, efficient access to the 4-amino-3-carboxamide disubstituted pyridine-2(1H)-one kinase hinge-binder motif proved to be more challenging than anticipated requiring a significant investment in route scouting and optimization. This full paper focuses on the synthesis issues that we encountered during our route exploration and the original solutions we found that helped us to identify two optimized library-style processes to prepare our large kinase inhibitor library.

中文翻译:

在室温下离子加氢条件下通过吡啶-2-氧基-7-氮杂苯并三唑醚的裂解来合成3,4-二取代的吡啶-2(1H)-酮的新型文库

在我们手中,事实证明,有效地使用4-氨基-3-羧酰胺双取代的吡啶-2(1 H)-一个激酶铰链结合基序比预期的更具挑战性,而这需要对路线搜寻和优化进行大量投资。这篇完整的论文重点介绍了我们在路线探索过程中遇到的合成问题以及我们发现的原始解决方案,这些解决方案有助于我们识别出两种优化的文库式流程,以制备大型激酶抑制剂文库。
更新日期:2021-01-18
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