On December 31, 2014, Liu, Hong; Dai, Xing; Palani, Anandan; He, Shuwen; Nargund, Ravi; Xiao, Dong; Dang, Qun; Peng, Xuanjia; Li, Peng published a patent.Synthetic Route of 1256359-96-2 The title of the patent was Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases. And the patent contained the following:
Title compounds I [X = pyridinone, pyrimidinone, pyridazone, etc.; B = (un)substituted 5- to 6-membered monocyclic ring, 9- to 10-membered bicyclic ring or C(O)NHCR5R6; A = fluorophenyl; D = absent or NR3SO2R4; R2 = alkyl; R3 = alkyl; R4 = alkyl; R5 = H, alkyl, or hydroxyalkyl; R6 = H or R5 and R6 together with the carbon to which they are attached form cyclopropyl], and their pharmaceutically acceptable salts, are prepared and disclosed. Thus, e.g., II was prepared by Suzuki reaction of 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonylamino)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide with 5-bromo-1-methylpyridin-2(1H)-one followed by bromination and Suzuki reaction with 4-fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-lH-indole. Compounds of the invention were tested for their inhibitory activity using HCV replicon system, e.g., II showed IC50 value of 3.616 nM for genotypes 1a and 3.885 nM for genotype 1b. The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. The experimental process involved the reaction of 4-Fluoro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole(cas: 1256359-96-2).Synthetic Route of 1256359-96-2
The Article related to benzofuran preparation hcv viral disease, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Synthetic Route of 1256359-96-2
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles