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The invention discloses a method for synthesizing aromatic amine compound, characterized in that in accordance with the following two kinds of methods in any method for carrying out: method a: will have the general formula (I) of the alkyl aromatic compound having the general formula (II) with the nitrogen containing compound mixed, oxidizing agent and organic solvent in the presence of reaction under the condition of having the general formula (III) of the aromatic amine compound; the second method: will have the general formula (I ‘) of the aromatic alcohol derivatives having the general formula (II) with the nitrogen containing compound mixed, in the acid additive and the presence of organic solvent prepared through the reaction of the formula (III) of the aromatic amine compound. The invention of the first use of the bulk of the alkyl aromatic compound or aromatic alcohol derivatives as raw materials, under the action of the non-metal catalytic, produced by the reaction of aromatic amine compound, compared with the traditional synthetic method with high yield, condition is simple, less waste emissions, does not need metal involved in, the reaction apparatus is simple, easy to industrial production and the like, therefore, has a wide application. (by machine translation)

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H370O – PubChem

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Tuberculosis (TB) remains a major cause of mortality worldwide, and improved treatments are needed to combat emergence of drug resistance. Inosine 5?-monophosphate dehydrogenase (IMPDH), a crucial enzyme required for de novo synthesis of guanine nucleotides, is an attractive TB drug target. Herein, we describe the identification of potent IMPDH inhibitors using fragment-based screening and structure-based design techniques. Screening of a fragment library for Mycobacterium thermoresistible (Mth) IMPDH DeltaCBS inhibitors identified a low affinity phenylimidazole derivative. X-ray crystallography of the Mth IMPDH DeltaCBS-IMP-inhibitor complex revealed that two molecules of the fragment were bound in the NAD binding pocket of IMPDH. Linking the two molecules of the fragment afforded compounds with more than 1000-fold improvement in IMPDH affinity over the initial fragment hit.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H393O – PubChem

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Provided is a compound represented by the Formula (I) having a HER2 inhibitory action or a pharmacologically acceptable salt thereof, wherein T1 is a phenyl group, an indazolyl group, or a benzofuryl group, n is an integer of 0 to 3, R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or a C1-4 alkoxy group, m is an integer of 0 to 3, R2 is a hydroxy group or a C1-4 alkyl group optionally substituted with one or two C1-4 alkoxy groups, and R3 is a hydrogen atom, a C1-4 alkyl group, or a C2-6 alkynyl group.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H373O – PubChem

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The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.

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Benzofuran – Wikipedia,
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The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) alpha (NR1H3) and/or beta (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer’s disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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Benzofuran – Wikipedia,
Benzofuran | C8H362O – PubChem

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Two analogues of the discontinued tumor vascular-disrupting agent verubulin (Azixa, MPC-6827, 1) featuring benzo-1,4-dioxan-6-yl (compound 5 a) and N-methylindol-5-yl (compound 10) residues instead of the para-anisyl group on the 4-(methylamino)-2-methylquinazoline pharmacophore, were prepared and found to exceed the antitumor efficacy of the lead compound. They were antiproliferative with single-digit nanomolar IC50 values against a panel of nine tumor cell lines, while not affecting nonmalignant fibroblasts. Indole 10 surpassed verubulin in seven tumor cell lines including colon, breast, ovarian, and germ cell cancer cell lines. In line with docking studies indicating that compound 10 may bind the colchicine binding site of tubulin more tightly (Ebind=-9.8 kcal mol-1) than verubulin (E bind=-8.3 kcal mol-1), 10 suppressed the formation of vessel-like tubes in endothelial cells and destroyed the blood vessels in the chorioallantoic membrane of fertilized chicken eggs at nanomolar concentrations. When applied to nude mice bearing a highly vascularized 1411HP germ cell xenograft tumor, compound 10 displayed pronounced vascular-disrupting effects that led to hemorrhages and extensive central necrosis in the tumor. Variations on a promising theme: Tumor blood vessels are a good therapeutic target because they are fundamentally different from normal vasculature. This study shows that vascular-disrupting agents derived from verubulin have enhanced selectivity for cancer cells and lower general in vivo toxicity, yet they retain the strong antivascular activity of the lead compound.

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Benzofuran – Wikipedia,
Benzofuran | C8H385O – PubChem

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The N,N?-disubstituted cyanoguanidine is an excellent bioisostere of the thiourea and ketene aminal functional groups. We report the design and synthesis of a novel class of cyanoguanidine-based lactam derivatives as potent and orally active FXa inhibitors. The SAR studies led to the discovery of compound 4 (BMS-269223, Ki = 6.5 nM, EC2xPT = 32 muM) as a selective, orally bioavailable FXa inhibitor with an excellent in vitro liability profile, favorable pharmacokinetics and pharmacodynamics in animal models. The X-ray crystal structure of 4 bound in FXa is presented and key ligand-protein interactions are discussed.

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Benzofuran – Wikipedia,
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Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Compounds 11q and 11s are active in the SNL pain model with ED50s 3.3 and 6.4 mg/kg respectively. Metabolic outcome of propargyl amino moiety was studied.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H390O – PubChem

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The direct enantioselective synthesis of chiral azaheteroaryl ethylamines from vinyl-substituted N-heterocycles and anilines is reported. A chiral phosphoric acid (CPA) catalyst promotes dearomatizing aza-Michael addition to give a prochiral exocyclic aryl enamine, which undergoes asymmetric protonation upon rearomatization. The reaction accommodates a broad range of N-heterocycles, nucleophiles, and substituents on the prochiral centre, generating the products in high enantioselectivity. DFT studies support a facile nucleophilic addition based on catalyst-induced LUMO lowering, with site-selective, rate-limiting, intramolecular asymmetric proton transfer from the ion-paired prochiral intermediate.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H395O – PubChem

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The syntheses of 4-arylcarbonyl-amino-7-chloroquinolines (4-16), 4-N-arylamino-7-chloroquinolines (19-24), 1-(7-chloroquinolin-4-yl)-4-(2-pyridyl)piperazine (26) and 4-arylthio-7-chloro- (30-32, 35-38) and 4-arylsulphono-7-chloroquinolines (33, 34) have been carried out starting from 4,7-dichloroquinoline (1).The compounds have been tested for their blood schizontodicidal activity against Plasmodium berghei in mice and for anthelmintic activity against Ancylostoma ceylanicum in hamsters and Litomosoides carinii in cotton rats.However, none of the compounds tested shows any significant activity.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H381O – PubChem