[EN] TREATMENT OF OVARIAN CANCER WITH 2-AMINO-4H-NAPHTHO[1,2-b]PYRAN-3-CARBONITRILES<br/>[FR] TRAITEMENT DU CANCER DE L'OVAIRE PAR DES 2-AMINO-4H-NAPHTO[1,2-B]PYRAN-3-CARBONITRILES
申请人:SLOAN KETTERING INST CANCER
公开号:WO2013070998A1
公开(公告)日:2013-05-16
Methods for inhibiting the growth of ovarian cancer cells or other serosal cancer cells are disclosed. The method involves exposing the cells to a 2-amino-4H-naphtho[1,2-b]pyran-3-carbonitrile of formula. (I). wherein Y is CR1 or N and Z is CR5 or N.
Green chemistry approach: sodium fluoride-catalyzed highly efficient microwave irradiation-assisted synthesis of substituted chromene derivatives in aqueous medium
作者:K. Fabitha、C. G. Arya、Munugala Chandrakanth、Janardhan Banothu
DOI:10.1007/s11164-022-04929-w
日期:2023.3
applications in medicinal chemistry. The multicomponent Knoevenagel–Michael reaction is one of the most efficient strategies to construct these two scaffolds. Previous efforts have been made in converting the traditional organicsolvents to eco-friendly solvents including H2O generally in the presence of complex catalysts. Here we present our work of using sodium fluoride (NaF) as the catalyst to synthesize
2-Amino-4 H -benzo[ H ]chromene-3-carbonitrile 和 2-amino-5-oxo-4 H ,5 H -pyrano[3,2- c ]chromene-3-carbonitrile 是两个重要的药效团,具有广泛的在药物化学中的应用。多组分 Knoevenagel-Michael 反应是构建这两种支架的最有效策略之一。之前已经在将传统有机溶剂转化为包括 H 2在内的环保溶剂方面做出了努力O 通常在复杂的催化剂存在下。在这里,我们介绍了我们使用氟化钠 (NaF) 作为催化剂从 α-或 β-萘酚或 4-羟基香豆素开始合成范围广泛的两种底物的工作。在微波辐射条件下使用 12 mol% NaF,反应在 15-25 分钟内完成,所有产率均超过 85%。通过用H 2 O洗涤简单地纯化反应产物并且可以通过用MeOH结晶进一步纯化。对绿色化学相关参数的分析表明,目前