282547-37-9

Upstream product

• 4964-71-0 5-bromoquinoline 
• 57260-71-6 1-t-Butoxycarbonylpiperazine 

Downstream Products

• 117922-84-6 5-(1-piperazinyl)-quinoline 

Relevant academic research and scientific papers

Electrochemically Driven, Ni-Catalyzed Aryl Amination: Scope, Mechanism, and Applications

C-N cross-coupling is one of the most valuable and widespread transformations in organic synthesis. Largely dominated by Pd- and Cu-based catalytic systems, it has proven to be a staple transformation for those in both academia and industry. The current study presents the development and mechanistic understanding of an electrochemically driven, Ni-catalyzed method for achieving this reaction of high strategic importance. Through a series of electrochemical, computational, kinetic, and empirical experiments, the key mechanistic features of this reaction have been unraveled, leading to a second generation set of conditions that is applicable to a broad range of aryl halides and amine nucleophiles including complex examples on oligopeptides, medicinally relevant heterocycles, natural products, and sugars. Full disclosure of the current limitations and procedures for both batch and flow scale-ups (100 g) are also described.

Toll-like receptor-7 small molecule inhibitor and preparation method thereof

The invention belongs to the field of chemical small molecules, and particularly relates to a Toll-like receptor-7 small molecule inhibitor. The invention provides the Toll-like receptor-7 small molecule inhibitor, which takes a co-inhibitor of TLR7 and TLR8 obtained by screening as a research object, realizes selective regulation and control of TLR7 and TLR8 through the research on the structureoptimization and structure-activity relationship (SAR) of a parent compound, and further develops a high-efficiency, non-toxic and specific small molecule inhibitor with certain selectivity on TLR 7.The TLR7 small molecule inhibitor has a certain effect and potential medicinal value in autoimmune diseases (systemic lupus erythematosus).

ORGANOSILICON COMPOUNDS AND THEIR USE AS THE MODULATORS OF THE TRPV1 RECEPTOR

A compound having the Formula (1): wherein: X1, X2, X3 and X4 independently represent CH or N; R1, R2 and R3 independently represent C1-6 alkyl, C3-8 cycloalkyl or C3-8 cycloalky IC1-6alkyl, each of which groups may be optionally substituted with one or more substituents independently selected from halogen and haloC1-6 alkyl; R4, R5, R6, R7, R8 and R9 independently represent H, C1-6 alkyl, C3-8 cycloalkyl or -QI-OR14, or R4 and R9 may join to form a bridging C1-6 alkylene chain; R10 represents aryl or heteroaryl, each of which may be optionally substituted by one or more substituents, independently selected from halogen, C1-6 alkyl, haloC1-6 alkyl, hydroxyC1-6alkyl, haloC1-6 alkoxy, cyano, -Q2-CO2R12, -Q2-COR12, -Q2-CONR12R13, -Q2-OR12, -Q2-NR12Rn, -Q2-NR12SO2R13, -Q2- NR12COR13, -Q2-SO2NR12R13, -Q2-S(O)mR12, -Y-aryl, -Y-heteroaryl, -Y-C3-8 cycloalkyl and -Y-heterocyclyl; Q1 and Q2 independently represent a covalent bond, C1-6 alkylene, or 1-6 alkylene substituted with hydroxy; R12 and R13 independently represent a H atom, or a C1-6 alkyl or C3-8 cycloalkyl group, in which each group may be optionally substituted with one or more C1-6 alkoxy; or when R12 and R13 are attached to the same nitrogen atom they may join to form a nitrogen containing heterocyclyl ring, which may be optionally substituted with one or more substituents independently selected from C1-6 alkyl and C1-6 alkoxy; R14 represents a H atom, or a C1-6 alkyl or C3-8 cycloalkyl group, in which each group may be optionally substituted with one or more C1-6 alkoxy; Y represents a covalent bond, C1-6 alkylene, or -O-. m represents 0, 1 or 2; R11, which is optionally present and may be attached to any available carbon atom X1 to X4 instead of H, represents halogen, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, cyano or C1-6 alkyl which may be optionally substituted with one or more substituents independently selected from halogen, haloC1-6 alkyl and OR16; q represents 0, 1 or 2; W represents -(CH2)n-, which may be optionally substituted with one or more substituents independently selected from C1-6 alkyl, C3-8 cycloalkyl and -Q3-OR15; n represents 1 or 2; Q3 represents a covalent bond or C1-6 alkylene; R15 represents H, C1-6 alkyl, or C3-8 cycloalkyl; R16 is as defined for R14; or a pharmaceutically acceptable salt or ester thereof. Uses of the compounds as modulators of the TrpVl receptor are also disclosed.