revealed that Cu 2 O and CuI were deposited on the MWCNTs in the cubic and γ phases, respectively. These results also showed that the Cu-containing MWCNTs exhibited weak to strong electron-accepting (Lewis acidic) properties. The catalytic activities of these materials were studied for the synthesis of biologically significant N -(pyridin-2-yl)benzamides via the oxidative amidation of aryl aldehydes
摘要 使用湿浸渍法将 Cu 2 O 和 CuI 负载在多壁碳纳米管 (MWCNTs) 上,并通过粉末 X 射线衍射、傅里叶变换红外光谱、扫描电子显微镜和能量色散 X 射线光谱对所得材料进行了全面表征。 、透射电子显微镜和程序升温脱附与氨分析。这些实验的结果表明,Cu 2 O 和CuI 分别以立方相和γ 相沉积在MWCNT 上。这些结果还表明,含铜的多壁碳纳米管表现出弱到强的电子接受(路易斯酸性)特性。研究了这些材料的催化活性,用于通过芳基醛与 2-氨基吡啶的氧化酰胺化合成具有生物学意义的 N-(吡啶-2-基)苯甲酰胺。产物的产率在 50%–95% 的范围内,选择性为 100%。值得注意的是,就产物的分离产率而言,CuI/MWCNT 催化剂比 Cu 2 O/MWCNT 催化剂更有效,尽管这两种催化剂中的后者表现出更好的可回收性。与共价 CuI 相比,在酸活化 MWCNTs 的极性与离子 Cu
Process for the preparation of acalabrutinib
申请人:Apotex Inc.
公开号:US10800787B2
公开(公告)日:2020-10-13
The present invention provides processes for the preparation of Acalabrutinib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for coupling of a compound of Formula (5) and 2-butynoic acid in the presence of Carbodiimide (8) to afford Acalabrutinib (1).
Metal-free oxidative amidation of aldehydes with aminopyridines employing aqueous hydrogen peroxide
作者:E. Sankari Devi、Anitha Alanthadka、A. Tamilselvi、Subbiah Nagarajan、Vellaisamy Sridharan、C. Uma Maheswari
DOI:10.1039/c6ob01454b
日期:——
The first metal free report on the amidation of aldehydes with aminopyridines was accomplished using simple aqueoushydrogenperoxide (aq. H2O2) as the oxidant. No catalysts or additives were needed for this transformation and the reaction proceeded in water, an environmentally benign reaction medium. Green oxidant and reaction conditions, and the ability to construct diverse N-(pyridin-2-yl)benzamide
关于醛与氨基吡啶酰胺化的第一个无金属报告是使用简单的过氧化氢水溶液(H 2 O 2水溶液)作为氧化剂完成的。该转化不需要催化剂或添加剂,并且反应在环境友好的水介质中进行。绿色的氧化剂和反应条件,以及通过这种优美的方法构建各种N-(吡啶-2-基)苯甲酰胺的能力,使其成为合成这些酰胺的实用替代品。