1623751-79-0

Upstream product

• 96631-87-7 1H-indole-7-carbonitrile 
• 5720-07-0 4-methoxyphenylboronic acid 
• 1777-55-5 (4-methoxyphenacylidene)triphenyl phosphorane 
• 1623752-24-8 5-((tert-butyldimethylsilyl)oxy)-1-(4-methoxyphenyl)pent-2-en-1-one 
• 109-97-7 pyrrole 
• 1616777-25-3 (E)-4-diazo-5-(4-methoxyphenyl)-5-oxopent-2-enal 
• 1647059-16-2 C₁₂H₁₂N₂O₃ 
• 1647059-10-6 C₁₈H₂₆N₂O₃Si 

Relevant academic research and scientific papers

Anticancer active indole derivatives, synthetic method and use thereof

The present invention relates to an indole derivative and uses of the indole derivative in preparation of anti-cancer drugs for tumor inhibition, wherein a cyano indole compound and a boric acid compound can be subjected to one-step synthesis in the prese

Palladium-catalyzed direct addition of arylboronic acids to 2-aminobenzonitrile derivatives: Synthesis, biological evaluation and in silico analysis of 2-aminobenzophenones, 7-benzoyl-2-oxoindolines, and 7-benzoylindoles

A palladium-catalyzed direct addition of arylboronic acids to unprotected 2-aminobenzonitriles has been developed, leading to a wide range of 2-aminobenzophenones with moderate to excellent yields. The transformation has broad scope and high functional group tolerance. Moreover, 2-oxoindoline-7-carbonitrile and indole-7-carbonitrile were applicable to this process for the construction of 7-benzoyl-2-oxoindolines and 7-benzoylindoles, respectively. Among the compounds examined, compound 4e possessed the most potent anticancer activity against H446 and HGC-27 in vitro, with IC50 values of 0.02 μmol L-1 and 0.09 μmol L-1, respectively, while compound 4a showed the best potent anticancer activity against SGC-7901 with an IC50 value of 0.01 μmol L-1. Furthermore, we also performed in silico molecular docking calculations to investigate the interaction mode and binding affinity between the examined compounds and their tubulin target. This journal is

Rhodium enalcarbenoids: Direct synthesis of indoles by rhodium(II)- catalyzed [4+2] benzannulation of pyrroles

Disclosed herein is the design of an unprecedented electrophilic rhodium enalcarbenoid which results from rhodium(II)-catalyzed decomposition of a new class of enaldiazo compounds. The synthetic utility of these enalcarbenoids has been successfully demonstrated in the first transition-metal-catalyzed [4+2] benzannulation of pyrroles, thus leading to substituted indoles. The new benzannulation has been applied to the efficient synthesis of the natural product leiocarpone as well as a potent adipocyte fatty-acid binding protein inhibitor. Fat cat: A new class of enaldiazo compounds resulted in the first transition-metal-catalyzed [4+2] benzannulation of pyrroles to deliver indoles. The benzannulation is proposed to involve an unprecedented diacceptor rhodium enalcarbenoid. The reaction was used in the highly efficient synthesis of the natural product leiocarpone and a potent adipocyte fatty-acid binding protein inhibitor.