85704-08-1

Upstream product

• 699-03-6 N-methyl-4-bromobenzylamine 
• 75-36-5 acetyl chloride 
• 79-16-3 N-methyl-acetamide 
• 589-15-1 1-bromomethyl-4-bromobenzene 
• 127-19-5 N,N-dimethyl acetamide 
• 106-37-6 1.4-dibromobenzene 

Downstream Products

• 1421341-01-6 N-methyl-N-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)acetamide 

Relevant academic research and scientific papers

Photocatalytic (Het)arylation of C(sp3)-H Bonds with Carbon Nitride

Graphitic carbon nitride materials have attracted significant interest in recent years and found applications in diverse light-to-energy conversions such as artificial photosynthesis, CO2 reduction, or degradation of organic pollutants. However, their utilization in synthetic photocatalysis, especially in the direct functionalization of C(sp3)-H bonds, remains underexplored. Herein, we report mesoporous graphitic carbon nitride (mpg-CN) as a heterogeneous organic semiconductor photocatalyst for direct arylation of C(sp3)-H bonds in combination with nickel catalysis. Our protocol has a broad synthetic scope (>70 examples including late-stage functionalization of drugs and agrochemicals), is operationally simple, and shows high chemo- and regioselectivities. Facile separation and recycling of the mpg-CN catalyst in combination with its low preparation cost, innate photochemical stability, and low toxicity are beneficial features overcoming typical shortcomings of homogeneous photocatalysis. Detailed mechanistic investigations and kinetic studies indicate that an unprecedented energy-transfer process (EnT) from the organic semiconductor to the nickel complex is operating.

THERAPEUTIC INHIBITORY COMPOUNDS

The invention provides compounds of Formula I and Formula II: A-B-C-D-E-F-G-J (I) C-D-E-F-G-J (II) wherein A, B, C, D, E, F, G, and J have any of the values defined in the specification, and salts thereof. The compounds are useful for inhibiting plasma kallikrein, and for treating a disease or condition in an animal where inhibition of plasma kallikrein is indicated.

SUBSTITUTED QUINOLINES AND THEIR USE AS MEDICAMENTS

The invention relates to new substituted quinolines of formula (1) wherein R1 is a linear or branched C1-6-alkyl, wherein R1 may optionally be substituted by R3 which is selected from the group consisting of a three-, four-, five-, six- or seven-membered cycloalkl; a five-, six- or seven-membered, saturated heterocycle comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; and a five- or six-membered heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; wherein R3 may optionally be substituted further substituted as defined in claim 1 and wherein R2 is selected from the group consisting of halogen, phenyl, a five- or six-membered monocyclic heteroaryl comprising one, two or three heteroatoms each independently selected from the group consisting of N, S and O; a bicyclic, nine-, ten- or eleven-membered, either aromatic or non-aromatic, but not fully saturated heterocycle comprising one, two, three or four heteroatoms each independently selected from the group consisting of N, S and O; wherein R2 may optionally be further substituted as defined in claim 1, and their use in the preparation of medicaments for the treatment of disease such as asthma, COPD, allergic rhinitis, allergic dermatitis and rheumatoid arthritis.

Substituted Quinolines and Their Use As Medicaments

Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.

Integration of lead optimization with crystallography for a membrane-bound ion channel target: Discovery of a new class of AMPA receptor positive allosteric modulators

A novel series of AMPAR positive modulators is described that were identified by high throughput screening. The molecules of the series have been optimized from a high quality starting point hit to afford excellent developability, tolerability, and effica

CHEMICAL COMPOUNDS-576

The invention relates to chemical compounds of the formula (I): or pharmaceutically or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of trea

COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE

Compounds of formula (I) and salts and solvates are provided: formula (I). Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.