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• 3466-32-8 4-bromoohenyl methyl sulfone 
• 62-53-3 aniline 
• 52323-93-0 1-methanesulfonyl-4-methylsulfanyl-benzene 

Relevant academic research and scientific papers

Nickel-Catalyzed Amination of (Hetero)aryl Halides Facilitated by a Catalytic Pyridinium Additive

An efficient and operationally simple Ni-catalyzed amination protocol has been developed. This methodology features a simple NiII salt, an organic base and catalytic amounts of both a pyridinium additive and Zn metal. A diverse number of (hetero)aryl halides were coupled successfully with primary and secondary alkyl amines, and anilines in good to excellent yields. Similarly, benzophenone imine gave the corresponding N-arylation product in an excellent yield.

Nickel-Catalyzed Amination of Aryl Thioethers: A Combined Synthetic and Mechanistic Study

Herein, we report a nickel-1,2-bis(dicyclohexylphosphino)ethane (dcype) complex for the catalytic Buchwald-Hartwig amination of aryl thioethers. The protocol shows broad applicability with a variety of different functional groups tolerated under the catalytic conditions. Extensive organometallic and kinetic studies support a nickel(0)-nickel(II) pathway for this transformation and revealed the oxidative addition complex as the resting state of the catalytic cycle. All the isolated intermediates have proven to be catalytically and kinetically competent catalysts for this transformation. The fleeting transmetalation intermediate has been successfully synthesized through an alternative synthetic organometallic pathway at lower temperature, allowing for in situ NMR study of the C-N bond reductive elimination step. This study addresses key factors governing the mechanism of the nickel-catalyzed Buchwald-Hartwig amination process, thus improving the understanding of this important class of reactions.

AMINO-SUBSTITUTED AZO-HETEROCYCLIC COMPOUNDS FOR TREATING INFLAMMATORY CONDITIONS

Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein X1 is -S-, -O-, -N=N-. -NR5-, -CR5=CR6-, -CR5=N-, wherein R5 and R6 are independently hydrogen or C1-C3 alkyl; R1 is hydrogen or C1-C3 alkyl or cyclopropyl; R2 is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring; R3 is an optionally substituted carbocyclic ring of 3 to 7 ring atoms, or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; R4 is a group other than hydrogen, methyl or ethyl of formula Q-[Alk1]m-[X]n-[Alk2]p-[Z}s- wherein m, n p, and s are independently 0 or 1 ; Q is hydrogen or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; Alk1 and Alk2 are independently optionally substituted C1-C3 alkylene radicals; X is -O-, -S-, -C(=O)-, - S(=O)-, -S(=O)2-, -CH(R7)-, -N(R7)-, or, in either orientation -SO2N(R7)- or - C(=O)N(R7)-, wherein R7 is hydrogen, or R7 represents a C2-C4 bridge between the C or N atom of X to which it is attached and a carbon atom of Alk2 and Z is -CH2, - C(=O) or -S(=O)2.