857594-97-9

Upstream product

• 53312-77-9 2-amino-3-chlorobenzonitrile 
• 56762-32-4 1-(2-amino-3-chlorophenyl)ethan-1-one 
• 2065-66-9 methyl-triphenylphosphonium iodide 
• 1779-49-3 Methyltriphenylphosphonium bromide 
• 608-31-1 2,6-Dichloroaniline 
• 59772-49-5 2-bromo-6-chloroaniline 
• 126726-62-3 2-isopropenyl-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane 

Relevant academic research and scientific papers

K-RAS G12C inhibitor as well as preparation method and application thereof

The invention relates to a K-RAS G12C inhibitor with a structure shown in a formula (I) as well as a preparation method and application of the K-RAS G12C inhibitor. A series of the compounds can be widely applied to preparation of drugs for treating tumors or cancers at least partially mediated by K-RAS G12C mutation, especially drugs for treating lung, liver and gall, gastrointestinal tract, blood system, skin, bone, urogenital tract, nervous system, gynecological and adrenal gland related malignant tumors or cancers, and are expected to be developed into a new generation of K-RAS G12C inhibitor drugs.

SULFONIMIDAMIDE COMPOUNDS AS NLRP3 MODULATORS

Described herein are compounds of Formula (I), Formula (I-A), and Formula (I-B), solvates thereof, tautomers thereof, and pharmaceutically acceptable salts of the foregoing, Further described herein are methods of inhibiting NLRP3 using said compounds, and methods of and compositions useful in treating NLRP3-dependent disorders.

MACROCYCLIC SULFONYLAMIDE DERIVATIVES USEFUL AS NLRP3 INHIBITORS

The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyl amides. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

Experimental and Computational Studies on Cp*CyRh(III)/KOPiv-Catalyzed Intramolecular Dehydrogenative Cross-Couplings for Building Eight-Membered Sultam/Lactam Frameworks

Described herein is an unusual Cp*CyRh(III)-catalyzed intramolecular site-specific aryl C-H annulation, a highly chemoselective protocol providing direct access to eight-membered sultams/lactams with broad substrate/functional group tolerance. Experimental and computational studies reveal that such a transformation involves a unique PivOH-assisted aryl C-H activation/alkene insertion/β-H elimination/hydrogen-transfer process involving the Rh(III)-hydride species as the active intermediate with the concomitant release of H2 as the major byproduct, thus enabling the developed Cp*CyRh(III) catalysis with redox-neutral and highly atom-economical features.

Water-Soluble Hypervalent Iodine(III) Having an I-N Bond. A Reagent for the Synthesis of Indoles

A readily accessible and bench-stable water-soluble hypervalent iodine(III) reagent (phenyliodonio)sulfamate (PISA) with an I-N bond was synthesized, and its structure was characterized by X-ray crystallography. With PISA, various indoles were synthesized via C-H amination of 2-alkenylanilines involving an aryl migration/intramolecular cyclization cascade with excellent regioselectivity in aqueous CH3CN. Notably, using this new method as the key step, not only two drug molecules, indometacin and zidometacin, but also another bioactive molecule, pravadoline, were synthesized.