107737-89-3

Upstream product

• 14703-92-5 4-(2-hydroxyethylthio)bromobenzene 
• 106-53-6 para-bromobenzenethiol 
• 857787-82-7 1,2-bis-(4-bromo-benzenesulfonyl)-ethane 

Downstream Products

• 122865-52-5 2-(4-bromophenylsulphonyl)ethyl chloroformate 
• 700870-27-5 4-(2-hydroxyethylsulfonyl)styrene 
• 1404060-99-6 C₈H₇BrO₃S 
• 22898-07-3 1-bromo-4-(vinylsulfonyl)benzene 
• 1200573-23-4 2-({4-[2-(1-benzoylpiperidin-4-yl)-4H-1,3-benzodioxin-6-yl]phenyl}sulfonyl)ethanol 
• 122865-60-5 N-<2-(4-bromophenylsulphonyl)ethoxycarbonyl>-L-trytophan dimethylamide 
• 122885-16-9 2-(4-bromophenylsulphonyl)ethyl succinimido carbonate 
• 90561-24-3 <4-Bromphenyl>-<2-methylsulfonyloxy-aethyl>-sulfon 

Relevant academic research and scientific papers

A new approach to the synthesis of 4-hydroxyethylsulfonylstyrene

A new, more environmentally benign route to hydroxyethylsulfonylstyrene has been developed, starting from 4-bromobenzenethiol, involving a solventless thioether formation, water-based perborate oxidation, and Suzuki-Miyaura cross coupling with a vinylborate reagent.

NEW COMPOUND

PROBLEM TO BE SOLVED: To provide a new compound that does not have structural similarity to ceramide and has excellent CERT inhibitory activity. SOLUTION: The present invention provides a new compound of structural formula (I). A bond group -X- is cis-cyclopropyl-, R1, R2, R3, R4, and R5 independently represent a hydrogen atom, a halogen atom, a linear or branched C1-C8 alkyl group that may have a halogen atom, or OR6. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT

DIPHENYL DERIVATIVES AND USES THEREOF

The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

INDOLE DERIVATIVES AND USES THEREOF

The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeleta

INHIBITING ATAXIA TELANGIECTASIA AND RAD3-RELATED PROTEIN (ATR)

Novel compounds inhibiting ATR protein kinase include compounds of formula (I) disclosed herein, as well as liposome formulations comprising ATR protein kinase inhibitor compounds. The compositions are useful for the treatment of cancer.

Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4′-(3- methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916)

The design of a new clinical candidate histamine-H3 receptor antagonist for the potential treatment of excessive daytime sleepiness (EDS) is described. Phenethyl-R-2-methylpyrrolidine containing biphenylsulfonamide compounds were modified by re

Design, Synthesis, and Evaluation of 2-(arylsulfonyl)oxiranes as Cell-permeable Covalent Inhibitors of Protein Tyrosine Phosphatases

A structure-based design approach has been applied to develop 2-(arylsulfonyl)oxiranes as potential covalent inhibitors of protein tyrosine phosphatases. A detailed kinetic analysis of inactivation by these covalent inhibitors reveals that this class of compounds inhibits a panel of protein tyrosine phosphatases in a time- and dose-dependent manner, consistent with the covalent modification of the enzyme active site. An inactivation experiment in the presence of sodium arsenate, a known competitive inhibitor of protein tyrosine phosphatase, indicated that these inhibitors were active site bound. This finding is consistent with the mass spectrometric analysis of the covalently modified protein tyrosine phosphatase enzyme. Additional experiments indicated that these compounds remained inert toward other classes of arylphosphate-hydrolyzing enzymes, and alkaline and acid phosphatases. Cell-based experiments with human A549 lung cancer cell lines indicated that 2-(phenylsulfonyl)oxirane (1) caused an increase in intracellular pTyr levels in a dose-dependent manner thereby suggesting its cell-permeable nature. Taken together, the newly identified 2-(arylsulfonyl)oxiranyl moiety could serve as a novel chemotype for the development of activity-based probes and therapeutic agents against protein tyrosine phosphatase superfamily of enzymes.

PROCESS FOR THE PREPARATION OF 2- [VINYL (HETERO) ARYL SULPHONYL] ETHANOL DERIVATIVES

The present invention relates to a method of making monomers of the formula X=C (H) -Y-S02-CH2-CH (R) -OH which comprises reacting a compound of the formula Q-Y-S02-CH2-CH (R) -OH with a vinyl-containing organometallic reagent comprising a substituted or unsubstituted moiety X=, wherein X= is a group selected from CH2=, MeO2C(H)C=, MeO2C(Me)C= and MeC02C=; Y is an optionally substituted aromatic or heteroaromatic diradical; R is a hydrogen or Cl-5 alkyl group; and Q is bromo, chioro, iodo, triflate or tosylate. These monomers are of utility in the preparation of cross-linkable resin compositions

New base-labile amino-protective groups for peptide synthesis

Modification of the methyl group in 2-(methylsulphonyl)ethanol gave alcohols which could be used to introduce amino-protective groups of the urethane type, which are labile in alkaline media.The cleavage involves β-elimination.Exchange of the methyl group by a phenyl group bearing a function with a negative inductive effect (NO2 or MeSO2) afforded protecting groups with a higher sensitivity to base.The recommended function is a disulphone: 2-ethanol.The function has a somewhat better stability than the Fmoc group, resists catalytic hydrogenolysis, is highly stable in acidic medium and its elimination product does not polymerize spontaneously.The suggested designation of the new protective group is Mpc.