855196-51-9

Upstream product

• 22133-40-0 4-aminophenyl propyl sulphide 
• 151-50-8 potassium cyanide 
• 540-54-5 1-Chloropropane 
• 49584-26-1 p-cyanobenzenesulfonyl chloride 
• 26891-63-4 1-propyl-2'-thiopyridine 
• 6068-72-0 4-cyanobenzoyl chlorIde 
• 619-65-8 4-cyanobenzoic Acid 
• 1194-02-1 4-fluorobenzonitrile 
• 6898-84-6 sodium 1-propanethiolate 
• 623-00-7 4-bromobenzenecarbonitrile 

Downstream Products

• 857489-11-3 4-propylsulfanyl-benzoic acid amide 
• 855290-50-5 4-(propylsulfonyl)benzonitrile 
• 22683-48-3 4-(propylthio)benzoic acid 

Relevant academic research and scientific papers

Ni-Catalyzed Aryl Sulfide Synthesis through an Aryl Exchange Reaction

A Ni-catalyzed aryl sulfide synthesis through an aryl exchange reaction between aryl sulfides and a variety of aryl electrophiles was developed. By using 2-pyridyl sulfide as a sulfide donor, this reaction achieved the synthesis of aryl sulfides without using odorous and toxic thiols. The use of a Ni/dcypt catalyst capable of cleaving and forming aryl-S bonds was important for the aryl exchange reaction between 2-pyridyl sulfides and aryl electrophiles, which include aromatic esters, arenol derivatives, and aryl halides. Mechanistic studies revealed that Ni/dcypt can simultaneously undergo oxidative additions of aryl sulfides and aromatic esters, followed by ligand exchange between the generated aryl-Ni-SR and aryl-Ni-OAr species to furnish aryl exchanged compounds.

BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ROR-GAMMA

Provided are novel compounds of Formula I: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by RORy. Also provided are pharmaceutical compositions comprising the novel compounds of Formula I and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

CuI promoted sulfenylation of organozinc reagents with arylsulfonyl chlorides

A CuI promoted sulfenylation of organozinc reagents with arylsulfonyl chlorides/PPh3 has been explored. This reaction proceeded smoothly through an alkyl/aryl radical (generated from organometallics) under mild conditions and produced the desired sulfide products in excellent yields.

Thioetherification via Photoredox/Nickel Dual Catalysis

Hypervalent alkylsilicates represent new and readily accessible precursors for the generation of alkyl radicals under photoredox conditions. Alkyl radicals generated from such silicates serve as effective hydrogen atom abstractors from thiols, furnishing thiyl radicals. The reactive sulfur species generated in this manner can be funneled into a nickel-mediated cross-coupling cycle employing aromatic bromides to furnish thioethers. The serendipitous discovery of this reaction and its utilization for the thioetherification of various aryl and heteroaryl bromides with a diverse array of thiols is described. The S-H selective H atom abstraction event enables a wide range of functional groups, including those bearing protic moieties, to be tolerated. (Chemical Equation Presented).

THERAPEUTIC AGENTS

A compound of the formula (I): wherein R1,R2,R3, R4,Ar, A, n and m are defined herein, is disclosed as a GlyT1 inhibitor; pharmaceutical compositions containing the compound of the formula (I) are also disclosed as are their use in medicine, for example in the treatment of schizophrenia.