313336-66-2Relevant academic research and scientific papers
A catalytic method for synthesizing α - one amide compound
-
Paragraph 0127; 0128; 0129, (2018/08/23)
The invention discloses a catalytic carbonylation method for synthesis of alpha-keto amide. A palladium source in an aqueous solution of polyethylene glycol or polyethylene glycol is used for in-situ formation of a highly active palladium nano-catalyst; a
Ligand-Free Pd-Catalyzed Double Carbonylation of Aryl Iodides with Amines to α-Ketoamides under Atmospheric Pressure of Carbon Monoxide and at Room Temperature
Du, Hongyan,Ruan, Qing,Qi, Minghao,Han, Wei
supporting information, p. 7816 - 7823 (2015/08/18)
A general Pd-catalyzed double carbonylation of aryl iodides with secondary or primary amines to produce α-ketoamides at atmospheric CO pressure has been developed. This transformation proceeds successfully even at room temperature and in the absence of any ligand and additive. A wide range of aryl iodides and amines can be coupled to the desired α-ketoamides in high yields with excellent chemoselectivities. Importantly, the current methodology has been demonstrated to be applied in the synthesis of bioactive molecules and chiral α-ketoamides.
Palladium-catalyzed mono- and double-carbonylation of indoles with amines controllably leading to amides and α-ketoamides
Xing, Qi,Shi, Lijun,Lang, Rui,Xia, Chungu,Li, Fuwei
supporting information, p. 11023 - 11025 (2013/01/15)
A novel and efficient double-carbonylation of indoles with primary or secondary amines to yield indole-3-α-ketoamides has been developed and bioactive molecules could be one-pot synthesized using the current methodology, which could also be selectively switched to mono-carbonylation to afford indole-3-amides only by a slight modification of reaction conditions.
Inhibitors of HIV-1 attachment. Part 2: An initial survey of indole substitution patterns
Meanwell, Nicholas A.,Wallace, Owen B.,Fang, Haiquan,Wang, Henry,Deshpande, Milind,Wang, Tao,Yin, Zhiwei,Zhang, Zhongxing,Pearce, Bradley C.,James, Jennifer,Yeung, Kap-Sun,Qiu, Zhilei,Kim Wright,Yang, Zheng,Zadjura, Lisa,Tweedie, Donald L.,Yeola, Suresh,Zhao, Fang,Ranadive, Sunanda,Robinson, Brett A.,Gong, Yi-Fei,Wang, Hwei-Gene Heidi,Blair, Wade S.,Shi, Pei-Yong,Colonno, Richard J.,Lin, Pin-fang
scheme or table, p. 1977 - 1981 (2009/11/30)
The effects of introducing simple halogen, alkyl, and alkoxy substituents to the 4, 5, 6 and 7 positions of 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione, an inhibitor of the interaction between HIV gp120 and host cell CD4 receptors, on activity in an HIV entry assay was examined. Small substituents at C-4 generally resulted in increased potency whilst substitution at C-7 was readily tolerated and uniformly produced more potent HIV entry inhibitors. Substituents deployed at C-6 and, particularly, C-5 generally produced a modest to marked weakening of potency compared to the prototype. Small alkyl substituents at N-1 exerted minimal effect on activity whilst increasing the size of the alkyl moiety led to progressively reduced inhibitory properties. These studies establish a basic understanding of the indole element of the HIV attachment inhibitor pharmacophore.
