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Upstream product

• 91-21-4 1,2,3,4-tetrahydroisoquinoline 
• 201230-82-2 carbon monoxide 
• 19501-58-7 4-methoxyphenylhydrazine hydrochloride 
• 5720-07-0 4-methoxyphenylboronic acid 
• 78823-41-3 C₁₃H₁₆O₄ 
• 100-09-4 4-methoxybenzoic acid 
• 100-07-2 4-methoxy-benzoyl chloride 

Relevant academic research and scientific papers

Green and environment-friendly method for synthesizing amide bonds

The invention provides a green and environment-friendly method for synthesizing amide bonds. The green and environment-friendly method includes forming C-Pd bonds from aryl hydrazine compounds under the oxidation effects of oxygen by the aid of palladium catalysts by means of oxidation hydrazine removal; carrying out carbonyl insertion reaction on the C-Pd bonds and carbon monoxide gas to generate palladium acyl species; feeding primary or secondary amine into palladium acyl and then carrying out reductive elimination to obtain a final product amide. The primary or secondary amine is used as a nucleophilic reagent. The green and environment-friendly method has the advantages that palladium catalytic carboamidation reaction is carried out on the aryl hydrazine compounds, normal-pressure CO is used as a carbonyl source for synthesizing the amide, and byproducts are nitrogen and water which are environmentally friendly; the green and environment-friendly method is novel and environmentally friendly, is high in efficiency and has great potential application value.

Palladium-Catalyzed Oxidative Carbonylation of Aryl Hydrazines with CO and O2 at Atmospheric Pressure

Palladium-catalyzed aerobic oxidative aminocarbonylation and alkoxycarbonylation reactions with aryl hydrazines as coupling partners have been developed. The oxidative carbonylation of aryl hydrazines proceeded smoothly at atmospheric pressure CO, employi

Dioxygen-promoted Pd-catalyzed aminocarbonylation of organoboronic acids with amines and CO: A direct approach to tertiary amides

A direct approach from organoboronic acids and amines to tertiary amides via Pd-catalyzed aerobic aminocarbonylation has been developed. The presence of O2 significantly promotes the efficiency of this transformation. This method uses commercially available organoboronic acids and cheap CO and O2 (1 atm), which renders amides an easy synthesis with broad substrate scope and high functional group tolerance.

Environment-friendly amido bond synthesis method

The invention discloses an environment-friendly amido bond synthesis method, which comprises the following steps: oxidizing an aryl hydrazine compound with O2 to form a C-Pd bond by taking Pd(OAc)2 as a catalyst and taking PPh3 as a ligand, inserting CO to a carbon-palladium bond to form an acyl palladium species as a carbonyl source, attacking carbonyl palladium by virtue of amine as a nucleophilic reagent, and performing reductive elimination to obtain a final product amide. According to the method, synthesis of the amide from the hydrazine compound is implemented by adopting CO as the carbonyl source by virtue of a carbonyl insertion method, and a byproduct does not comprise excessive pollutants such as haloid acid, so that the potential application value can be better achieved.

Direct inter- and intramolecular addition of amides to arylalkenes promoted by KOt-Bu/DMF

Direct addition of tetrahydroisoquinoline derived amides to arylalkenes has been achieved in the presence of KOt-Bu/DMF. Both intermolecular and intramolecular reactions could occur in good yields. α-Amido alkyl radicals are proposed to be generated under the reaction conditions. The reaction is efficient for the synthesis of seven-membered nitrogen heterocycles. A homoprotoberberine was prepared conveniently via this method.

COMPOUNDS AND METHODS FOR TREATING PROTEIN FOLDING DISORDERS

The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, Aβ protein or α-synuclein protein aggregation.