157187-14-9

Usage

Uses

Used in Pharmaceutical Industry:
1-Fluoro-4-(pyrrolidinosulfonyl)benzene is used as a key intermediate in the synthesis of pharmaceuticals for its potential pharmacological activity. It contributes to the development of new drugs by providing a versatile building block with unique structural features.
Used in Agrochemical Industry:
1-Fluoro-4-(pyrrolidinosulfonyl)benzene is used as a key intermediate in the synthesis of agrochemicals, enabling the development of novel compounds with improved efficacy and selectivity in crop protection and pest management.
Used in Organic Compounds Synthesis:
1-Fluoro-4-(pyrrolidinosulfonyl)benzene is used as a valuable building block for the synthesis of various organic compounds, leveraging its unique structural composition and reactivity to create new molecules with diverse applications.
Used in Functional Materials Production:
1-Fluoro-4-(pyrrolidinosulfonyl)benzene serves as a key intermediate in the production of various functional materials, such as advanced polymers, coatings, and adhesives, due to its versatile reactivity and structural properties.
Used in Fine Chemicals Industry:
1-Fluoro-4-(pyrrolidinosulfonyl)benzene is used as a key intermediate in the production of fine chemicals, which are high-purity, specialty chemicals used in various applications, including pharmaceuticals, fragrances, and flavorings. Its unique structure and reactivity contribute to the development of high-quality fine chemicals.

InChI:InChI=1/C10H12FNO2S/c11-9-3-5-10(6-4-9)15(13,14)12-7-1-2-8-12/h3-6H,1-2,7-8H2

Upstream product

• 123-75-1 pyrrolidine 
• 349-88-2 4-Fluorobenzenesulfonyl chloride 
• 2266-41-3 4-fluorobenzenesulfonylhydrazide 
• 7335-06-0 1-ethylpyrrolidine 
• 824-80-6 sodium 4-fluorobenzenesulfinate 

Downstream Products

• 882500-18-7 4-(pyrrolidin-1-ylsulfonyl)benzenethiol 
• 1383479-26-2 C₂₉H₃₂N₂O₅S 

Relevant academic research and scientific papers

Tetramethylammonium Fluoride Alcohol Adducts for SNAr Fluorination

Nucleophilic aromatic fluorination (SNAr) is among the most common methods for the formation of C(sp2)-F bonds. Despite many recent advances, a long-standing limitation of these transformations is the requirement for rigorously dry, aprotic conditions to maintain the nucleophilicity of fluoride and suppress the generation of side products. This report addresses this challenge by leveraging tetramethylammonium fluoride alcohol adducts (Me4NF·ROH) as fluoride sources for SNAr fluorination. Through systematic tuning of the alcohol substituent (R), tetramethylammonium fluoride tert-amyl alcohol (Me4NF·t-AmylOH) was identified as an inexpensive, practical, and bench-stable reagent for SNAr fluorination under mild and convenient conditions (80 °C in DMSO, without the requirement for drying of reagents or solvent). A substrate scope of more than 50 (hetero) aryl halides and nitroarene electrophiles is demonstrated.

Synthesis method of beta-aryl sulfonyl enamine compound

The invention belongs to the technical field of organic synthesis. The invention relates to the technical field of organic synthesis, in particular to a synthesis method of a beta-aryl sulfonyl enamine compound, which comprises the following steps: in an air environment, with a sodium benzenesulfinate derivative and tertiary amine as substrates, carrying out anodic oxidation coupling reaction in amixture of an electrolyte and a solvent to obtain the beta-aryl sulfonyl enamine compound. The synthesis method of the beta-aryl sulfonyl enamine compound provided by the invention is free of metal,oxidant and halogen, the whole synthesis process is harmless to the environment, and a variety of beta-aryl sulfonyl enamine compounds with satisfactory yield can be obtained.

Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships

Lysyl oxidase (LOX) is a secreted copper-dependent amine oxidase that cross-links collagens and elastin in the extracellular matrix and is a critical mediator of tumor growth and metastatic spread. LOX is a target for cancer therapy, and thus the search for therapeutic agents against LOX has been widely sought. We report herein the medicinal chemistry discovery of a series of LOX inhibitors bearing an aminomethylenethiophene (AMT) scaffold. High-throughput screening provided the initial hits. Structure-activity relationship (SAR) studies led to the discovery of AMT inhibitors with sub-micromolar half-maximal inhibitory concentrations (IC50) in a LOX enzyme activity assay. Further SAR optimization yielded the orally bioavailable LOX inhibitor CCT365623 with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy.

Iodine-catalyzed sulfonylation of sulfonyl hydrazides with: Tert -amines: A green and efficient protocol for the synthesis of sulfonamides

This study provides a direct, sustainable and eco-friendly method for the synthesis of various sulfonamides via the sulfonylation of sulfonyl hydrazides with tert-amines. The method utilizes sulfonyl hydrazides to oxidize and couple with tertiary amines through selective cleavage of C-N bonds. In this reaction, molecular iodine was used as the catalyst and t-butyl hydroperoxide was used as the oxidant.

TBAI-catalyzed selective synthesis of sulfonamides and β-aryl sulfonyl enamines: coupling of arenesulfonyl chlorides and sodium sulfinates with tert-amines

A simple, practical and metal-free method has been developed for the synthesis of sulfonamides and β-arylsulfonyl enamines via the selective cleavage of C-N and C-H bonds through the iodine-catalyzed oxidation of arenesulfonyl chlorides and sodium sulfinates with tert-amines. The method uses commercially available inexpensive catalysts and oxidants, and has a wide substrate scope and operational simplicity.

Method for synthesizing benzenesulfonamide compound by using benzenesulfonyl chloride compound and secondary amine through metal-free catalysis

The invention provides a method for synthesizing a benzenesulfonamide compound by using a benzenesulfonyl chloride compound and secondary amine through metal-free catalysis. The method comprises the following steps: taking the benzenesulfonamide compound

Method for synthesizing benzenesulfonamide compound by using benzenesulfonohydrazide derivative and secondary amine through metal-free catalysis

The invention provides a method for synthesizing a benzenesulfonamide compound by using a benzenesulfonohydrazide derivative and secondary amine through metal-free catalysis. The method comprises thefollowing steps: taking the benzenesulfonohydrazide deri

METHYLAMINE DERIVATIVES AS LYSYSL OXIDASE INHIBITORS FOR THE TREATMENT OF CANCER

Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

Synthesis of [18F]Fluoroarenes by Nucleophilic Radiofluorination of N-Arylsydnones

A practical method for radiofluorination of anilines with [18F]fluoride via N-arylsydnone intermediates is described. These precursors are stable, easy to handle and facilitate direct and regioselective 18F-labeling to prepare [

G-PROTEIN COUPLED RECEPTOR AGONISTS

Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.