383-23-3

Usage

Uses

Used in Pharmaceutical Development:
OTAVA-BB BB7011460335 is used as a potential ligand for various receptors in the central and peripheral nervous system, including dopamine, serotonin, and adrenergic receptors, for the development of new pharmaceuticals targeting neurological and psychiatric disorders.
Used in Neurological Disorders Treatment:
In the field of neurology, OTAVA-BB BB7011460335 is used as a potential therapeutic agent for the treatment of neurological disorders, leveraging its interaction with key receptors in the nervous system to modulate neurotransmission and alleviate symptoms.
Used in Psychiatric Disorders Treatment:
OTAVA-BB BB7011460335 is used as a potential therapeutic agent in psychiatry for the treatment of psychiatric disorders, where its psychoactive properties and receptor interactions may contribute to managing mental health conditions.
Used in Research and Testing:
In the scientific community, OTAVA-BB BB7011460335 is used as a subject of research and testing to better understand its potential uses, effects, and mechanisms of action, with the aim of advancing knowledge in the fields of neurology and psychiatry and informing the development of new treatments.

Upstream product

• 110-91-8 morpholine 
• 2905-15-9 1-fluoro-4-[(4-fluorobenzenesulfonyl)sulfanyl]benzene 
• 1828-66-6 morpholine-4-sulfonyl chloride 
• 1765-93-1 4-fluoroboronic acid 
• 352-13-6 4-flourophenylmagnesium bromide 
• 23328-69-0 4-chloromorpholine 
• 459-45-0 4-fluorobenzenediazonium tetrafluoroborate 
• 371-42-6 4-Fluorothiophenol 
• 5765-65-1 4-(benzoyloxy)morpholine 
• 651-07-0 4-fluorobenzenesulfonic acid sodium salt 
• 824-80-6 sodium 4-fluorobenzenesulfinate 
• 349-88-2 4-Fluorobenzenesulfonyl chloride 

Downstream Products

• 917761-20-7 bis[4-(morpholine-4-sulfonyl)benzene]disulfide 
• 1025712-36-0 1-cyclohexyl-6-(1-(4-(morpholinosulfonyl)phenyl)azetidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one 
• 785000-58-0 N-[4-(morpholin-4-ylsulfonyl)phenyl]guanidine 
• 53915-80-3 p-(sulphonylmorpholino)phenylhydrazine 

Relevant academic research and scientific papers

S(vi) in three-component sulfonamide synthesis: Use of sulfuric chloride as a linchpin in palladium-catalyzed Suzuki-Miyaura coupling

Sulfuric chloride is used as the source of the -SO2- group in a palladium-catalyzed three-component synthesis of sulfonamides. Suzuki-Miyaura coupling between the in situ generated sulfamoyl chlorides and boronic acids gives rise to diverse sulfonamides in moderate to high yields with excellent reaction selectivity. Although this transformation is not workable for primary amines or anilines, the results show high functional group tolerance. With the solving of the desulfonylation problem and utilization of cheap and easily accessible sulfuric chloride as the source of sulfur dioxide, redox-neutral three-component synthesis of sulfonamides is first achieved. This journal is

Efficient and Practical Synthesis of Sulfonamides Utilizing SO2 Gas Generated on Demand

A simple and practical protocol was developed for the synthesis of sulfonamides by reacting organometallic reagents with SO2 gas generated on demand. SO2 was generated from readily available reagents safely in a highly contained and controlled fashion. The protocol allows the synthesis of sulfonamides without using either atom-inefficient SO2 surrogates or a SO2 cylinder that requires stringent storage regulations in the laboratory. The protocol was successfully applied to the synthesis of sildenafil.

Synthesis of aromatic sulfonamides through a copper-catalyzed coupling of aryldiazonium tetrafluoroborates, DABCO·(SO2)2, and N-Chloroamines

A copper-catalyzed aminosulfonylation of aryldiazonium tetrafluoroborates, DABCO·(SO2)2, and N-chloroamines is described. This coupling reaction provides an efficient and simple approach to a wide range of sulfonamides in moderate to good yields under mild conditions. Mechanistic investigation suggests that a radical process and transition-metal catalysis are merged in this tandem reaction.

Direct Copper-Catalyzed Three-Component Synthesis of Sulfonamides

First introduced into medicines in the 1930s, the sulfonamide functional group continues to be present in a wide range of contemporary pharmaceuticals and agrochemicals. Despite their popularity in the design of modern bioactive molecules, the underpinning methods for sulfonamide synthesis are essentially unchanged since their introduction, and rely on the use of starting materials with preinstalled sulfur-functionality. Herein we report a direct single-step synthesis of sulfonamides that combines two of the largest monomer sets available in discovery chemistry, (hetero)aryl boronic acids and amines, along with sulfur dioxide, using a Cu(II) catalyst, to deliver a broad range of sulfonamides. Sulfur dioxide is provided by the surrogate reagent DABSO. The reaction tolerates broad variation in both coupling partners, including aryl, heteroaryl and alkenyl boronic acids, as well as cyclic and acyclic alkyl secondary amines, and primary anilines. We validate the method by showing that a variety of drugs, and drug-fragments, can be incorporated into the process.

MANUFACTURING METHOD OF COMPOUND HAVING SULFONYL GROUP

The present invention relates to a method for manufacturing a compound having a sulfonyl group, which includes a step for reacting thiosulfonates in a solvent comprising nucleophilic bases with an electrophilic agent. Accordingly, the present invention can manufacture the compound having the sulfonyl group with a variety of structures with high efficiency and high yield through more simplified processes than conventional methods.COPYRIGHT KIPO 2018

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 [

One-Pot Bimetallic Pd/Cu-Catalyzed Synthesis of Sulfonamides from Boronic Acids, DABSO and O-Benzoyl Hydroxylamines

A practical and straightforward bimetallic Pd/Cu catalytic system has been developed. This system affords various sulfonamides in one pot from easy-to-handle and readily available boronic acids, sulfur dioxide surrogate DABSO and O-benzoyl hydroxylamines in high yields. Without additional ligands, the newly developed catalytic system revealed a broad substrate scope for both partners and tolerated a wide array of functional groups even at low catalyst loadings. Furthermore, based on control experiments, a plausible mechanism has been proposed, in which sodium sulfinate has been isolated and identified as the crucial intermediate for this transformation.

Synthesis of Sulfones and Sulfonamides via Sulfinate Anions: Revisiting the Utility of Thiosulfonates

Simple and high-yielding strategies for the production of a variety of sulfones and sulfonamides, using thiosulfonates synthesized by copper-catalyzed aerobic dimerization, are reported. Although thiosulfonates are an old class of compound, practical methods for their synthesis and utilization have not been rigorously developed. In this study, we revisit the reactions of easily accessible thiosulfonates to form sulfinate anions. Because of the similar reactivity of thiosulfonates and metal sulfinates derived from toxic SO2, thiosulfinates are proposed to be stable, nontoxic alternatives to metal sulfinate salts.

Copper-Catalyzed Sulfonylation of Alkenes and Amines by Using Thiosulfonates as a Sulfonylating Agent

Synthetically and pharmaceutically useful vinyl sulfones and sulfonamides are synthesized by the direct coupling of thiosulfonates with alkenes and amines, respectively. Copper catalysts help to generate the sulfonyl group from thiosulfonates and to form the C(sp2)–S/N–S bonds of the organosulfur compounds. This paper discusses the scope of these reactions of aromatic and aliphatic thiosulfonates with alkenes and amines.

Metal-free I2O5-mediated direct construction of sulfonamides from thiols and amines

A simple and convenient method has been developed for the construction of sulfonamides via I2O5-mediated sulfonylation of amines with arylthiols. The present protocol provides an attractive approach to sulfonamides in moderate to good yields from readily accessible and easy to handle starting materials under mild and metal-free conditions.