122399-89-7

Upstream product

• 142-08-5 2-hydroxypyridin 
• 99-90-1 para-bromoacetophenone 
• 98-98-6 2-Picolinic acid 
• 99-93-4 4-Hydroxyacetophenone 
• 372-48-5 2-fluoropyridine 

Downstream Products

• 122399-85-3 2-Hydroxy-4-oxo-4-[4-(pyridin-2-yloxy)-phenyl]-butyric acid 
• 98-86-2 acetophenone 
• 1609173-95-6 ethyl 3-(4-(pyridin-2-yloxy)phenyl)-1H-pyrazole-5-carboxylate 
• 403-14-5 3-fluoro-4-hydroxyacetophenone 

Relevant academic research and scientific papers

Transition-Metal-Catalyzed Transformation of Sulfonates via S-O Bond Cleavage: Synthesis of Alkyl Aryl Ether and Diaryl Ether

The catalytic conversion of sulfonates, a versatile class of pharmaceutical intermediates, is usually based on C-O bond cleavage. In this paper, however, we discover a rare transformation of sulfonates via S-O bond cleavage catalyzed by transition metal, through which alkyl sulfonates could undergo an intramolecular desulfitative C-O coupling to form aryl alkyl ethers in the presence of a nickel catalyst. Meanwhile, aryl sulfonates perform similarly to give diaryl ethers catalyzed by a palladium complex. This transformation could tolerate a wide range of functionalities. Controlled experiments reveal that the 2-pyridyl group is necessary to promote the reaction as designed. Crossover experiments proved that this transformation might proceed partly in an intermolecular pathway.

Decarbonylative Diaryl Ether Synthesis by Pd and Ni Catalysis

Because diaryl ethers are present as an important motif in pharmaceuticals and natural products, extensive studies for the development of novel methods have been conducted. A conventional method for the construction of the diaryl ether moiety is the intermolecular cross-coupling reaction of aryl halides and phenols with a copper or palladium catalyst. We developed a catalytic decarbonylative etherification of aromatic esters using a palladium or nickel catalyst with our enabling diphosphine ligand to give the corresponding diaryl ethers. The present reaction can be conducted on gram scale in excellent yield. This reaction not only functions in an intramolecular setting but also allows for a cross-etherification using other phenols.

BTK INHIBITOR

Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).

Substituted pyridoimidazole derivative and preparation thereof, and applications of substituted pyridoimidazole derivative in medicines

The present invention discloses a substituted pyridoimidazole derivative and preparation thereof, and applications of the substituted pyridoimidazole derivative in medicines, and particularly relates to a new derivative represented by a general formula (I) and a pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the new derivative, and a preparation method of the new derivative. The present invention further discloses applications of the derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition containing the new derivative in Bruton tyrosine kinase inhibitors and in preparation of drugs for treatment and/or prevention of tumors, inflammations, and other diseases, wherein each substituent in the general formula (I) is defined in the specification. The formula (I) is defined in the specification.

Derivative with imidazopyridine, preparation method and application in medicine thereof

The invention discloses a derivative with imidazopyridine, a preparation method and application in medicine thereof. Concretely speaking, the invention relates to a novel derivative, medicinal salt of the derivative or pharmaceutical compositions containing the derivative, and the preparation method of the derivative showed in general formula (I). The invention also discloses application of the derivative, medicinal salt of the derivative or pharmaceutical compositions containing the derivative in Bruton tyrosine kinase inhibitor, preparing the medicine for treating or preventing tumor and inflammation diseases. Substituent groups in general formula (I) are identical to definitions in the specification (the structure is shown in the description).

Derivative having imidazopyrazines, preparation method and application thereof of derivative on medicine

The invention discloses a derivative having imidazopyrazines, a preparation method and an application thereof of the derivative on medicine. Concretely speaking, the invention relates to a novel derivative shown in a general formula (I) and its medicinal salt or a pharmaceutical composition containing the derivative, and its preparation method. The invention also discloses the derivative or its medicinal salt or an application of the pharmaceutical composition containing the derivative in a Bruton tyrosine kinase inhibitor, and in preparation of medicines for treating and/or preventing diseases such as tumour and inflammation. The substituent in the formula (I) has same definition in the specification.

With substituted pyrazine and imidazole derivatives, their preparation and their use in medicine (by machine translation)

The invention discloses a substituted pyrazine and imidazole derivatives, their preparation and their use in medicine. Specifically, the invention relates to a compound of general formula (I) indicated by the new derivative and its pharmaceutically acceptable salt or pharmaceutical composition containing the same, and its preparation method. The invention also discloses the derivative and its pharmaceutically acceptable salt or pharmaceutical composition containing the same in the Bruton tyrosine kinase inhibitors, and in preparing and treating and/or preventing tumor diseases such as inflammation of the application of the medicament. Wherein the general formula (I) of each substituent as defined in the specification. (by machine translation)

Copper complexes and their use

The invention relates to copper complexes of phosphorus compounds, to a process for their preparation and to their use in catalytic coupling reactions.