501892-55-3

Upstream product

• 15126-06-4 methyl 3-iodo-4-hydroxybenzoate 
• 1066-54-2 trimethylsilylacetylene 
• 99-96-7 4-hydroxy-benzoic acid 
• 37470-46-5 4-hydroxy-3-iodobenzoic acid 
• 35387-93-0 3-iodo-4-methoxy-benzoic acid methyl ester 
• 99-76-3 methyl 4-hydroxylbenzoate 

Downstream Products

• 108763-47-9 5-(methoxycarbonyl)benzo[b]furan 
• 501892-56-4 methyl 2-trimethylsilylbenzofuran-5-carboxylate 
• 90721-27-0 benzofuran-5-carboxylic acid 
• 501892-54-2 N-[(1S,2R,4R)-7-Azabicyclo[2.2.1]hept-2-yl]-1-benzofuran-5-carboxamide hydrochloride 
• 1334314-78-1 methyl 2-[1-(3,4,5-trimethoxyphenyl)vinyl]benzofuran-5-carboxylate 
• 1195960-33-8 methyl 3-Ethynyl-4-hydroxybenzoate 

Relevant academic research and scientific papers

Iridium-Catalyzed Intramolecular Cycloisomerization between Functionalized Alkyne with Aryl Vinyl Ether: Synthesis of 2-Vinyl-3-functionalized Methylbenzofurans

We have developed cycloisomerization between an aryl vinyl ether and a functionalized alkyne, such as silylalkyne, to give 2,3-disubstituted benzofuran derivatives using [IrCl(cod)]2, PCy3, and NaBArF4. This catalyst system not only catalyzes the above cycloisomerization but also isomerize a terminal olefin to give an aryl vinyl ether.

Biomimetic carbene cascades enabled imine derivative migration from carbene -bearing thiocarbamates

Inspired by the body circulation of Omeprazole (irreversible proton pump inhibitor), we disclose the carbene-triggered cascades for the synthesis of 2-aminobenzofuran derivatives from N-sulfonyl-1,2,3-triazoles or benzothioazole-bearing thiocarbamates, which represents an unprecedented imine derivative migration process. Furthermore, the desulfurizing reagent-free Barton-Kellogg-type reactions starting from N-sulfonyl-1,2,3-triazoles have also been achieved for the first time, and elemental sulfur is confirmed as a byproduct during this transformation. Both experimental data and DFT calculations further thoroughly explained the unique reactivity.

Indium(III)-Catalyzed Synthesis of Benzo[ b]furans by Intramolecular Hydroalkoxylation of ortho-Alkynylphenols: Scope and Mechanistic Insights

Indium(III) halides catalyze the hydroalkoxylation reaction of ortho-alkynylphenols to afford benzo[b]furans in good yields. The reaction proceeds with 5-endo-dig regioselectivity with a variety of phenols functionalized at the arene and alkyne moieties in high yields using InI3 (5 mol %) in DCE. Experimental and computational studies support a mechanism based on the indium(III) π-Lewis acid activation of the alkyne followed by nucleophilic addition of the phenol and final protodemetalation to afford the corresponding benzo[b]furan. DFT calculations suggest that dimer In2I6 is the catalytic species through a novel double coordination with the alkyne and the hydroxyl group.

Imidazole-containing condensed tricyclic compound and application thereof

The invention discloses an imidazole-containing condensed tricyclic compound adopting the structure as shown in the formula (I) or pharmaceutically acceptable salts, stereisomers or prodrug molecules thereof. The imidazole-containing condensed tricyclic compound has the IDO1 activity regulation function, can enhance T-cell activation through blocking immune checkpoints IDO1, is used for treating IDO1-mediated immunosuppression, and therefore, can become an effective medicine for treating malignant tumors. When used together with checkpoint protein anti-body drugs or other anti-cancer drugs, the imidazole-containing condensed tricyclic compound can enhance the anti-cancer effect. Meanwhile, the imidazole-containing condensed tricyclic compound has the potential of effectively treating IDO1 abnormity related immunosuppressive diseases and has a high application value.

COMPOUNDS HAVING BOTH α7 NICOTINIC AGONIST ACTIVITY AND 5HT3 ANTAGONIST ACTIVITY FOR TREATMENT OF CNS DISEASES

The invention discloses compounds that are selective α7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.

Substituted 7-aza[2.2.1]bicycloheptanes for the treatment of disease

The invention provides compounds of Formula I: which may be in the form of pharmaceutical acceptable salts or compositions, are useful in treating diseases or conditions in which α7 nicotinic acetylcholine receptors (nAChRs) are known to be involved.

Azabicyclic compounds for the treatment of disease

The invention provides compounds of Formula I: 1wherein Azabicyclo is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which α7 is known to be involved.