81038-34-8Relevant academic research and scientific papers
Design, synthesis and evaluation of dihydropyranoindole derivatives as potential cholinesterase inhibitors against Alzheimer's disease
Shaikh, Sarfaraz,Pavale, Ganesh,Dhavan, Pratik,Singh, Pinky,Uparkar, Jasmin,Vaidya,Jadhav,Ramana
, (2021)
A series of novel dihydropyranoindole derivatives containing sulphonamide group were designed, synthesized and evaluated for in-vitro anti-cholinesterase activity. The result showed that all the compounds exhibited potent acetylcholinesterase (AChE) activ
Metal-free directed sp 2-C–H borylation
Lv, Jiahang,Chen, Xiangyang,Xue, Xiao-Song,Zhao, Binlin,Liang, Yong,Wang, Minyan,Jin, Liqun,Yuan, Yu,Han, Ying,Zhao, Yue,Lu, Yi,Zhao, Jing,Sun, Wei-Yin,Houk, Kendall. N.,Shi, Zhuangzhi
, p. 336 - 340 (2019/11/14)
Organoboron reagents are important synthetic intermediates that have a key role in the construction of natural products, pharmaceuticals and organic materials1. The discovery of simpler, milder and more efficient approaches to organoborons can
Application of E1cB Elimination in Asymmetric Organocatalytic Cascade Reactions to Construct Polyheterocyclic Compounds
You, Zhi-Hao,Chen, Ying-Han,Tang, Yu,Liu, Yan-Kai
supporting information, p. 8358 - 8363 (2019/10/16)
By introducing a carbon functionality at 2-position of chromane, the formal asymmetric functionalization of the 3-position of 2-substituted chromane has been realized via a highly chemo-, regio-, and stereoselective organocatalytic cascade reaction in a sequential one-pot manner involving an E1cB mechanism governed ring-opening process. Critical to our success was the design of a chiral dipeptide-based bifunctional acid-base organocatalyst, which exhibited high catalytic activity at low catalyst loading (1-0.1 mol %), leading to biologically interesting polyheterocyclic compounds.
The synthetic and biological studies of discorhabdins and related compounds
Wada, Yasufumi,Harayama, Yu,Kamimura, Daigo,Yoshida, Masako,Shibata, Tomoyuki,Fujiwara, Kousaku,Morimoto, Koji,Fujioka, Hiromichi,Kita, Yasuyuki
scheme or table, p. 4959 - 4976 (2011/08/06)
Various analogues of the marine alkaloids, discorhabdins, have been synthesized. The strategy contains spirocyclization with phenyliodine(iii) bis(trifluoroacetate) (PIFA), oxidative fragmentation of the β-amino alcohols with the hypervalent iodine reagent C6F 5I(OCOCF3)2, the detosylation and dehydrogenation reaction of the pyrroloiminoquinone unit in the presence of a catalytic amount of NaN3 and the bridged ether synthesis with HBr-AcOH as the key reactions. All the synthesized compounds were evaluated by in vitro MTT assay for cytotoxic activity against the human colon cancer cell line HCT-116. Furthermore, the discorhabdin A oxa analogues were also evaluated against four kinds of tumor model cells, a human colon cancer cell line (WiDr), a human prostate cancer cell line (DU-145) and murine leukemia cell lines (P388 and L1210). For the identification of the target, discorhabdin A and the discorhabdin A oxa analogue were evaluated by an HCC panel assay. In the test, discorhabdins could have a novel mode of action with the tumor cells. The Royal Society of Chemistry 2011.
Preparation of alkyl-substituted indoles in the benzene portion. Part 6. Synthetic procedure for 4-, 5-, 6-, or 7-alkoxy-and hydroxyindole derivatives
Fuji,Muratake,Natsume
, p. 2344 - 2352 (2007/10/02)
A novel method for the preparation of indole derivatives that are alkoxy- and hydroxy-substituted in the benzene portion of the indole nucleus is described. The acid-induced cyclization reaction of (arylsulfonyl)pyrrole derivatives (4a, 4b, 5b, and 5a) in
Selective halogenation of 4-oxo-4,5,6,7-tetrahydroindoles to 5-halo-4-oxo-4,5,6,7-tetrahydroindoles with copper(II) halides
Matsumoto, Masakatsu,Ishida, Yasuko,Watanabe, Nobuko
, p. 165 - 170 (2007/10/02)
Halogenation of 4-oxo-4,5,6,7-tetrahydroindoles with copper(II) bromide or copper(II) chloride gave selectively 5-halo-4-oxo-4,5,6,7-tetrahydroindoles, which were easily transformed to 4-hydroxyindoles by the action of lithium halide/lithium carbonate in
