58534-95-5

Usage

Uses

Used in Pharmaceutical Industry:
3-Bromo-2-fluoroaniline is used as a key intermediate in the synthesis of heterotricyclic carboxamides, which serve as RIG-I agonists. These agonists are important for the treatment of cell proliferation disorders, as they help modulate the immune response and have potential therapeutic applications in various diseases.
Used in Chemical Synthesis:
3-Bromo-2-fluoroaniline is also utilized as a building block in the preparation of other complex organic molecules and compounds. Its unique combination of bromine and fluorine atoms allows for a range of synthetic applications, including the development of new materials with specific properties for various industries.

InChI:InChI=1/C6H5BrFN/c7-4-2-1-3-5(9)6(4)8/h1-3H,9H2

Upstream product

• 848440-23-3 (3-bromo-2-fluorophenyl)carbamic acid tert-butyl ester 
• 161957-56-8 3-bromo-2-fluorobenzoic acid 
• 58534-94-4 2-fluoro-3-bromonitrobenzene 

Downstream Products

• 1184298-53-0 N-(3-bromo-2-fluoro-phenyl)-4-chloro-butyramide 
• 1386459-75-1 3-cyclopropyl-2-fluoroaniline 
• 1269233-04-6 N-(3-bromo-2-fluorophenyl)propane-1-sulfonamide 

Relevant academic research and scientific papers

Preparation and application of indolizine compound

The invention provides an indolizine compound for inhibiting a CBP/EP300Bromodomain receptor as well as a preparation method and application of the indolizine compound. The indolizine compound has a structure as shown in a formula I; the indolizine compound provided by the invention can be effectively combined with a CBP/EP300 bromodomain, and has good selectivity on other bromodomain family proteins; meanwhile, the indolizine compound provided by the invention is more stable in structure.

Discovery of selective fragment-sized immunoproteasome inhibitors

Proteasomes contribute to maintaining protein homeostasis and their inhibition is beneficial in certain types of cancer and in autoimmune diseases. However, the inhibition of the proteasomes in healthy cells leads to unwanted side-effects and significant effort has been made to identify inhibitors specific for the immunoproteasome, especially to treat diseases which manifest increased levels and activity of this proteasome isoform. Here, we report our efforts to discover fragment-sized inhibitors of the human immunoproteasome. The screening of an in-house library of structurally diverse fragments resulted in the identification of benzo[d]oxazole-2(3H)-thiones, benzo[d]thiazole-2(3H)-thiones, benzo[d]imidazole-2(3H)-thiones, and 1-methylbenzo[d]imidazole-2(3H)-thiones (with a general term benzoXazole-2(3H)-thiones) as inhibitors of the chymotrypsin-like (β5i) subunit of the immunoproteasome. A subsequent structure-activity relationship study provided us with an insight regarding growing vectors. Binding to the β5i subunit was shown and selectivity against the β5 subunit of the constitutive proteasome was determined. Thorough characterization of these compounds suggested that they inhibit the immunoproteasome by forming a disulfide bond with the Cys48 available specifically in the β5i active site. To obtain fragments with biologically more tractable covalent interactions, we performed a warhead scan, which yielded benzoXazole-2-carbonitriles as promising starting points for the development of selective immunoproteasome inhibitors with non-peptidic scaffolds.

Indolizine compound as well as preparation method and application thereof

The invention provides an indolizine compound as well as a preparation method and application thereof. The indolizine compound has a structure as shown in a formula I or a formula II, the indolizine compound can be effectively combined with a CBP/EP300 bromine structural domain, the inhibition rate can generally reach 90% or above, the indolizine compound has a good effect and has good selectivityon other bromine structural domain family proteins; moreover, the indolizine compound is stable in structure, and the synthesis method is simpler.

TYK2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Quinazoline compound and application thereof in medicine (by machine translation)

The invention relates to a quinazoline compound (shown in the formula I) and a medicinal salt thereof, which can be used for treating cancer. The invention also relates to a preparation method and a pharmaceutical composition containing the compounds. (by machine translation)

Small-compound enhancers for functional O-mannosylation of alpha-dystroglycan, and uses thereof

The present invention provides compounds that can enhance functional O-mannosylation of proteins including alpha-dystroglycan. Also provided are methods of preparation of the compounds defined by the formula I. Also provided are the methods of using the compounds or the pharmaceutical acceptable salts or prodrugs thereof in treating and preventing subjects suffering from the diseases including muscular dystrophies and cancers.

CONJUGATES OF CEREBLON BINDING COMPOUNDS AND G12C MUTANT KRAS, HRAS OR NRAS PROTEIN MODULATING COMPOUNDS AND METHODS OF USE THEREOF

Conjugates of a cereblon-binding compound and compounds having modulatory activity against G12C mutant KRAS, HRAS or NRAS G12C proteins are provided. Methods associated with preparation and use of such conjugates, pharmaceutical compositions comprising such conjugates and methods to modulate the activity of G12C mutant KRAS, HRAS or NRAS G12C proteins for treatment of disorders, such as cancer, are also provided.

SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF G12C MUTANT KRAS, HRAS AND/OR NRAS PROTEINS

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2c, A, B, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

2-SUBSTITUTED QUINAZOLINE COMPOUNDS COMPRISING A SUBSTITUTED HETEROCYCLIC GROUP AND METHODS OF USE THEREOF

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, G1, G2, L1, L2, m1, m2, n, X and E are as defined herein, and wherein at least one of R3a, R3b, R4a or R4b is not H. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

INHIBITORS OF KRAS G12C MUTANT PROTEINS

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, B R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.