115663-39-3

Upstream product

• 5446-92-4 2-methoxy-5-nitropyridine 
• 7205-98-3 chloromethyl phenyl sulfone 

Downstream Products

• 633304-65-1 3-Amino-6-methoxy-2-[(phenylsulfonyl)methyl]-pyridine 

Relevant academic research and scientific papers

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT6 receptor ligands

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which 6f and 6g showed high affinity for 5-HT6 receptors with Ki = 3.9 and 1.7 nM, respectively.

Reactions of nitroheteroarenes with carbanions: Bridging aromatic, heteroaromatic and vinylic electrophilicity

The relative rate constants for the vicarious nucleophilic substitution (VNS) of the anion of chloromethyl phenyl sulfone (1-) with a variety of nitroheteroarenes, for example, nitropyridines, nitropyrroles, nitroimidazoles, 2-nitrothiophene, and 4-nitropyrazole, have been determined by competition experiments. It was shown that nitropyridines are approximately four orders of magnitude more reactive than nitrobenzene. Among the five-membered heterocycles 2-nitrothiophene is the most active followed by nitroimidazoles and 4-nitropyrazole. Nitropyrroles are the least electrophilic nitroheteroarenes with reactivities comparable to nitrobenzene. Quantum chemically calculated methyl anion affinities (B3LYP/6-311 G(d,p)//B3LYP/ 6-31G(d)) of the nitroarenes correlated only moderately with the partial relative rate constants. The correlation of these activities with the LUMO energies of nitroarenes is even worse. By measuring the second-order rate constants of the addition of 1" to nitroarenes and to diethyl arylidenemalonates 10, it was possible to link the electrophilic reactivities of nitroheteroarenes with the comprehensive electrophilicity scale based on the linear-free-energyrelationship log k(20°C) = s(N + E).

1-(aminoalkyl)-3-sulfonylazaindoles as 5-hydroxytryptamine-6 ligands

The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

1-(AMINOALKYL)-3-SULFONYLAZAINDOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS

The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Influence of conjugation on orientation in substituted nitropyridines: Vicarious nucleophilic substitution of hydrogen with chloromethyl phenyl sulfone

2-Hydroxy- and 2-mercapto-5-nitropyridines as well as their O- (and S-) substituted derivatives enter Vicarious Nucleophilic Substitution of Hydrogen (VNS) with chloromethyl phenyl sulfone The orientation of the substitution can be controlled by varying the O- (or S-) substituent. The results of VNS in 4-methoxy-3-nitropyridine and 3-methoxy-2-nitropyridine are also reported.