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.
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Paragraph 00279; 00344
(2020/06/10)
Decarboxylative acylation of: N -free indoles enabled by a catalytic amount of copper catalyst and liquid-assisted grinding
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.
Yu, Jingbo,Zhang, Chao,Yang, Xinjie,Su, Weike
supporting information
p. 4446 - 4451
(2019/05/16)
INDOLE COMPOUNDS AND THEIR USE
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.
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Paragraph 00191; 00218; 00283
(2019/06/05)
Synthesis of 3-aroylindoles as intermediates of cannabimimetics and elucidation of their physicochemical properties
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
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.
Shi, Qing,Li, Pinhua,Zhu, Xianjin,Wang, Lei
p. 4916 - 4923
(2016/11/04)
Synthesis of 3-acylindoles by palladium-catalyzed acylation of free (N-H) indoles with nitriles
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.