727-95-7Relevant academic research and scientific papers
METHODS OF TREATING CANCER
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Paragraph 00279; 00344, (2020/06/10)
The present disclosure relates to methods of treating cancer in a patient using a combination of an inhibitor of an immune checkpoint protein and an indole compound or its phosphate derivative.
Decarboxylative acylation of: N -free indoles enabled by a catalytic amount of copper catalyst and liquid-assisted grinding
Yu, Jingbo,Zhang, Chao,Yang, Xinjie,Su, Weike
supporting information, p. 4446 - 4451 (2019/05/16)
A facile decarboxylative acylation of N-free indoles with α-ketonates via liquid-assisted grinding was reported. The reaction requires only a catalytic amount of Cu(OAc)2·H2O in combination with O2 as the terminal oxidant to give various 3-acylindoles with high efficiency. Additionally, this new methodology was applicable to a gram-scale synthesis.
INDOLE COMPOUNDS AND THEIR USE
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Paragraph 00191; 00218; 00283, (2019/06/05)
The present disclosure relates to indole compounds and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer.
Synthesis of 3-aroylindoles as intermediates of cannabimimetics and elucidation of their physicochemical properties
Araki, Koji,Makino, Kosho,Tabata, Hidetsugu,Nakayama, Hiroshi,Zaitsu, Kei,Oshitari, Tetsuta,Natsugari, Hideaki,Takahashi, Hideyo
, p. 910 - 920 (2018/06/07)
In order to synthesize the intermediates of cannabimimetics, the benzoylation of indoles with 2'/3'/4'-substituted benzoyl chloride in the presence of Et2AlCl was examined. Among the products, we found that the1H NMR spectra of 3-(2'-substitute
Decarboxylative/decarbonylative C3-acylation of indoles: Via photocatalysis: A simple and efficient route to 3-acylindoles
Shi, Qing,Li, Pinhua,Zhu, Xianjin,Wang, Lei
, p. 4916 - 4923 (2016/11/04)
A simple and efficient strategy for the preparation of 3-acylindoles via visible-light promoted C3-acylation of free (NH)- and N-substituted indoles with α-oxocarboxylic acids was developed. The reaction tolerates a wide range of functional groups, and the corresponding 3-acylindoles were obtained in high yields under mild conditions.
Synthesis of 3-acylindoles by palladium-catalyzed acylation of free (N-H) indoles with nitriles
Jiang, Tao-Shan,Wang, Guan-Wu
supporting information, p. 788 - 791 (2013/03/29)
An efficient palladium-catalyzed synthesis of 3-acylindoles using free (N-H) indoles and nitriles has been developed. The acylation reaction proceeded well under the Pd(OAc)2/2,2′-bipyridine system and with d-(+)-camphorsulfonic acid as the additive. A possible mechanism involving carbopalladation of nitriles and subsequent hydrolysis of ketimines is proposed.
