481630-48-2Relevant academic research and scientific papers
Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT6R ligands binding mode
Staroń, Jakub,Bugno, Ryszard,Pietru?, Wojciech,Sata?a, Grzegorz,Mordalski, Stefan,Warszycki, Dawid,Hogendorf, Agata,Hogendorf, Adam S.,Kalinowska-T?u?cik, Justyna,Lenda, Tomasz,Pilarski, Bogus?aw,Bojarski, Andrzej J.
supporting information, (2020/10/26)
Among all of the monoaminergic receptors, the 5-HT6R has the highest number of non-basic ligands (approximately 5% of compounds stored in 25th version of ChEMBL database have the strongest basic pKa below 5, calculated using the Instant JChem c
Rhodium(II)-Catalyzed [4+3] Cyclization of Triazoles with Indole Derivatives and Its Application in the Total Synthesis of (±)-Aurantioclavine
Duan, Shengguo,Xue, Bing,Meng, Hui,Ye, Zihang,Xu, Ze-Feng,Li, Chuan-Ying
supporting information, p. 1145 - 1152 (2021/04/26)
An efficient rhodium(II)-catalyzed [4+3] cyclization reaction of 1-sulfonyl-1,2-3-triazoles and indoles was developed. Azepino[5,4,3- cd]indoles, which are widely distributed in ergot alkaloids with various biological activities, could be obtained in good
The palladium-catalyzed direct C3-cyanation of indoles using acetonitrile as the cyanide source
Feng, Kejun,Li, Qiang,Li, Yuanhua,Liu, Bifu,Liu, Min,Zhou, Yongbo
supporting information, p. 6108 - 6114 (2020/10/21)
The ligand-free palladium-catalyzed C3-cyanation of indoles via direct C-H functionalization was achieved. This protocol, utilizing CH3CN as a green and readily available cyanide source, produced the desired products in moderate to good yields through transition-metal-catalyzed C-CN bond cleavage. This journal is
Efficient direct 2,2,2-trifluoroethylation of indoles via C-H functionalization
Tolnai, Gergely L.,Székely, Anna,Makó, Zita,Gáti, Tamás,Daru, János,Bihari, Tamás,Stirling, András,Novák, Zoltán
supporting information, p. 4488 - 4491 (2015/03/18)
A novel highly C3 selective metal free trifluoroethylation of indoles using 2,2,2-trifuoroethyl(mesityl)-iodonium triflate was developed. The methodology enables the introduction of a trifluoroethyl group in a fast and efficient reaction under mild conditions with high functional group tolerance. Beyond the synthetic developments, quantum chemical calculations provide a deeper understanding of the transformation. This journal is
Synthesis of tetracyclic indoles via intramolecular α-arylation of ketones
Hellal, Malik,Singh, Shambhavi,Cuny, Gregory D.
experimental part, p. 4123 - 4130 (2012/06/17)
Figure Persented: An intramolecular palladium(0)-mediated α-arylation of ketones applied to the synthesis of various substituted tetracyclic indoles is reported. Most significantly, the efficiency of the transformation was enhanced by the use of monoligated Pd(0) complexes. This methodology was extended to double α-arylation of ketones using one-pot reactions with either simultaneous addition or sequential addition of two aryl halides for producing aryl substituted tetracyclic indoles.
Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
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, (2008/06/13)
This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, —CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
