343238-31-3Relevant academic research and scientific papers
Construction of N-C Axial Chirality through Atroposelective C-H Olefination of N-Arylindoles by Palladium/Amino Acid Cooperative Catalysis
Zhang, Jitan,Xu, Qiaoqiao,Wu, Jiaping,Fan, Jian,Xie, Meihua
, p. 6361 - 6365 (2019/08/20)
Direct construction of N-C axial chirality via Pd-catalyzed atroposelective C-H olefination of N-arylindoles is reported. The crucial role of chiral amino acid as a cocatalyst in the regio- and stereocontrol has been disclosed. In this reaction, a wide range of arylindoles and functional alkenes could be well tolerated. Moreover, the practicality and synthetic value of this process were demonstrated by the divers and simple transformations of the products.
Efficient preparation method of 3-substitued-benzo five-membered heterocycle-2-carbonyl compound
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, (2017/08/30)
The invention discloses an efficient compounding method of a 3-substitued-benzo five-membered heterocycle-2-carbonyl compound. According to the method, a 3-substitued-benzo five-membered heterocycle-2-alcohol compound is subjected to a halogenated oxidation reaction by a halogenating reagent to generate the corresponding 3-substitued-benzo five-membered heterocycle-2-carbonyl compound. The efficient compounding method has the advantages that raw materials are easy to get, reaction conditions are mild, and reaction selectively and yield are high.
Fluorination-Oxidation of 2-Hydroxymethylindole Using Selectfluor
Jiang, Xiaojian,Zhang, Feng,Yang, Junjie,Yu, Pei,Yi, Peng,Sun, Yewei,Wang, Yuqiang
supporting information, p. 853 - 858 (2017/03/11)
An unexpected fluorination-oxidation of 2-hydroxymethylindole using selectfluor under mild condi-tions without a catalyst is described. This new chemistry allows for efficient and rapid synthesis of various 3-fluoroindole-2-aldehydes and novel quaternary
Facile Synthesis of 3-Halobenzo-heterocyclic-2-carbonyl Compounds via in situ Halogenation-Oxidation
Jiang, Xiaojian,Yang, Junjie,Zhang, Feng,Yu, Pei,Yi, Peng,Sun, Yewei,Wang, Yuqiang
supporting information, p. 2678 - 2683 (2016/09/03)
A facile method to synthesize 3-halobenzo-heterocyclic-2-carbonyl compounds is described. Mechanistic studies suggested that a halo-cyclization process, which generated the unstable spiro-acetal transition state and readily convertible to the corresponding carbonyl compound might be involved. Diverse 3-halobenzo-heterocyclic-2-carbonyl compounds could be synthesized with up to 95 % yield in mild conditions with inexpensive starting materials. (Figure presented.).
Design, synthesis and aromatase inhibitory activities of novel indole-imidazole derivatives
Wang, Rui,Shi, Hong-Fan,Zhao, Jing-Feng,He, Yan-Ping,Zhang, Hong-Bin,Liu, Jian-Ping
, p. 1760 - 1762 (2013/04/10)
A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and any bulky group should be avoided in order to keep a relative small volume for this kind of molecules.
