3285-31-2

Usage

Uses

Used in Pharmaceutical Industry:
2-BROMO-5-CHLOROSULFONYL-BENZOIC ACID is used as a building block for the synthesis of various pharmaceuticals. Its unique structure and properties allow for the creation of new drug molecules with potential therapeutic applications.
Used in Agrochemical Industry:
In the agrochemical sector, 2-BROMO-5-CHLOROSULFONYL-BENZOIC ACID is utilized as a precursor in the development of agrochemicals. Its reactivity and functional groups contribute to the production of effective compounds for crop protection and pest control.
Used in Dye Industry:
2-BROMO-5-CHLOROSULFONYL-BENZOIC ACID is employed as a key intermediate in the synthesis of dyes. Its chemical properties enable the creation of a wide range of colorants used in various industries, including textiles, plastics, and printing.
Used as a Reagent in Organic Synthesis:
Due to its strong electron-withdrawing properties, 2-BROMO-5-CHLOROSULFONYL-BENZOIC ACID is used as a reagent in the synthesis of other compounds. It can facilitate various chemical reactions, leading to the formation of new molecules with diverse applications.
Used in Materials Science:
2-BROMO-5-CHLOROSULFONYL-BENZOIC ACID has potential applications in materials science, where its unique properties can be harnessed to develop new materials with specific characteristics, such as improved stability or enhanced performance.
Used as a Research Tool in Chemical and Biological Studies:
In academic and research settings, 2-BROMO-5-CHLOROSULFONYL-BENZOIC ACID serves as a valuable tool for studying chemical and biological processes. Its reactivity and functional groups can provide insights into various reaction mechanisms and help advance our understanding of complex systems.

Upstream product

• 88-65-3 2-bromobenzoic-acid 
• 109-05-7 2-Methylpiperidin 

Downstream Products

• 1219139-80-6 2-bromo-5-(indole-1-sulfonyl) benzoic acid 
• 1429347-18-1 2-bromo-5-(N-(4-ethylphenyl)-N-isobutylsulfamoyl)benzoic acid 
• 1474110-21-8 N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide 
• 1219139-30-6 1-[4-bromo-3-(4-ethylpiperazin-1-yl-methyl)phenylsulfonyl]-5-methoxy-1H-indole 
• 1219139-29-3 1-[4-bromo-3-(4-methylpiperazin-1-yl-methyl)phenylsulfonyl]-5-methoxy-1H-indole 
• 1219139-31-7 1-[4-bromo-3-(4-ethylpiperazin-1-yl-methyl)phenylsulfonyl]-5-fluoro-1H-indole 

Relevant academic research and scientific papers

Nucleophilic Aromatic Substitutions of 2-Halo-5-(sulfamoyl)benzoic Acids and N, O-Bis-alkylation via Phase Transfer Catalysis: Synthesis of RoRγInverse Agonist GSK2981278A

GSK2981278A (1) is a RORγinverse agonist used as a potential topical nonsteroidal therapy for psoriasis. New synthesis of 1 was developed based on a SNAr reaction of (tetrahydro-2H-pyran-4-yl)methanol with an aryl halide intermediate, prepared from 2-halobenzoic acids. The dianion underwent in situ N,O-bis-isobutylation, followed by a reduction to provide 1. The new route eliminated a genotoxic tosylate of (tetrahydro-2H-pyran-4-yl)methanol and a difficult reductive amination from the original synthesis starting from methyl salicylate. A primary version of the route has been scaled up to deliver 125 kg of 1. However, the heating of a strong base in DMSO for an extended period during the bis-alkylation was found to be a safety concern for manufacturing. A safer and greener process was then developed utilizing a facile N,O-bis-alkylation, which was conducted under phase transfer conditions with mild bases such as potassium carbonate and in green solvents such as water. The concise four stage sequence from 2-halobenzoic acids to GSK2981278A (1) had an overall yield of 41%.

Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides

DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The enzyme poly(ADP-ribose) glycohydrolase (PARG) plays a pivotal role in the regulation of DNA repair mechanisms; however, the lack of potent drug-like inhibitors for use in cellular and in vivo models has limited the investigation of its potential as a novel therapeutic target. Using the crystal structure of human PARG in complex with the weakly active and cytotoxic anthraquinone 8a, novel quinazolinedione sulfonamides PARG inhibitors have been identified by means of structure-based virtual screening and library design. 1-Oxetan-3-ylmethyl derivatives 33d and 35d were selected for preliminary investigations in vivo. X-ray crystal structures help rationalize the observed structure-activity relationships of these novel inhibitors.

2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

BIOREVERSABLE PROMOIETIES FOR NITROGEN-CONTAINING AND HYDROXYL-CONTAINING DRUGS

Disclosed are promoieties of the following formula which can be used to form prodrugs of nitrogen-containing or hydroxyl-containing drug or a pharmaceutically active agent: (I) and pharmaceutical compositions comprising the prodrugs.

Chemical Compounds

The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.

Aromatic sulfonyl fluorides covalently kinetically stabilize transthyretin to prevent amyloidogenesis while affording a fluorescent conjugate

Molecules that bind selectively to a given protein and then undergo a rapid chemoselective reaction to form a covalent conjugate have utility in drug development. Herein a library of 1,3,4-oxadiazoles substituted at the 2 position with an aryl sulfonyl fluoride and at the 5 position with a substituted aryl known to have high affinity for the inner thyroxine binding subsite of transthyretin (TTR) was conceived of by structure-based design principles and was chemically synthesized. When bound in the thyroxine binding site, most of the aryl sulfonyl fluorides react rapidly and chemoselectively with the pK a-perturbed K15 residue, kinetically stabilizing TTR and thus preventing amyloid fibril formation, known to cause polyneuropathy. Conjugation t50s range from 1 to 4 min, ～1400 times faster than the hydrolysis reaction outside the thyroxine binding site. X-ray crystallography confirms the anticipated binding orientation and sheds light on the sulfonyl fluoride activation leading to the sulfonamide linkage to TTR. A few of the aryl sulfonyl fluorides efficiently form conjugates with TTR in plasma. Eleven of the TTR covalent kinetic stabilizers synthesized exhibit fluorescence upon conjugation and therefore could have imaging applications as a consequence of the environment sensitive fluorescence of the chromophore.

THERAPEUTICALLY ACTIVE COMPOUNDS FOR USE IN THE TREATMENT OF CANCER CHARACTERIZED AS HAVING AN IDH MUTATION

Compounds and compositions comprising compounds useful in the treatment of cancer are described herein. The compounds and compositions can be used to modulate an isocitrate dehydrogenase (IDH) mutant (e.g., IDHIm or IDH2m) having alpha hydroxyl neoactivity

Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: Structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109

Following the discovery of a new series of benzimidazole derivatives bearing a diarylmethyl group as inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase (HCV NS5B RdRp), we extended the structure-activity relationship (SAR) study to analogue

ANTIBACTERIAL AGENTS

The present invention relates to antibacterial agents that are useful for sterilization, sanitation, antisepsis, and disinfection.

Sulfamylbenzoic acids

Certain mono- and disubstituted-5-sulfamylbenzoic acids, many of which are novel, and their use in lowering blood lipid levels in mammals.