55114-91-5

Upstream product

• 577-19-5 2-nitrophenyl bromide 
• 16807-37-7 5-methoxy-2-sulfanyl-benzoic acid 
• 6705-03-9 2-Amino-5-methoxybenzoic acid 

Downstream Products

• 55114-92-6 2-amino-2'-carboxy-4'-methoxy-diphenylsulfide 
• 1004534-33-1 5-methoxy-2-(2-nitrophenylthio)-N,N-dimethylbenzamide 
• 1004534-40-0 5-hydroxy-2-(2-nitrophenylthio)-N,N-dimethylbenzamide 

Relevant academic research and scientific papers

Synthesis and evaluation of 2-(2′-((dimethylamino)methyl)-4′-(2-fluoroethoxy-substituted)phenylthio)benzenamine derivatives as potential positron emission tomography imaging agents for serotonin transporters

A series of diphenylsulfide derivatives with various substitutions at the 4-position on phenyl ring A and different lengths of the 2-fluoroethoxy-substituted side-chain at the 4′-position on ring B were synthesized and evaluated as potential positron emission tomography (PET) imaging agents for serotonin transporters (SERT). These ligands exhibited high SERT binding affinities (Ki = 0.11–1.3 nM) and the 4-methyl-substituted (4-Me) compounds 7a and 8a displayed excellent selectivity for SERT versus norepinephrine transporters (NET) (392- and 700-fold, respectively). In the parallel artificial membrane permeability assay (PAMPA), these ligands demonstrated moderate to high brain penetration, and the 4-Me analogs showed higher BBB permeability than the corresponding 4-F analogs. The 2-fluoroethoxy-substituted ligands showed higher metabolic stability and lower lipophilicity than 4-F-ADAM. [18F]7a-c were readily prepared using an automatic synthesizer and exhibited significant uptake and slow washout in rat brains. At 120 min after iv injection, [18F]7a exhibited the highest uptake in the midbrain, whereas [18F]7b exhibited the highest uptake in the hypothalamus and midbrain. After treatment with citalopram, a SERT-selective ligand, the uptake of [18F]7a in the hypothalamus and striatum was significantly decreased. The potent and highly selective SERT binding and the selective and reversible accumulation in SERT-rich brain regions suggested that [18F]7a is a promising lead for the further development of novel [18F]-labeled PET imaging agents for SERT binding sites in the brain.

2-(2′-((Dimethylamino)methyl)-4′-(fluoroalkoxy)-phenylthio) benzenamine derivatives as serotonin transporter imaging agents

A novel series of ligands with substitutions at the 5-position on phenyl ring A and at the 4′-position on phenyl ring B of 2-(2′- ((dimethylamino)methyl)-4′-(fluoroalkoxy)phenylthio)benzenamine (4′-2-fluoroethoxy derivatives 28-31 and 4′-3-fluoropropoxy d

PROCESS FOR PRODUCING DIBENZOTHIAZEPINE DERIVATIVES

A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f] [1,4]thiazepin-11-one employable as a starting material for the preparation of 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperadinyldiberizothiazepine derivative which is known to be effective as an antipsychotic pharmaceutical, has the steps of reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the obtained 2-nitro-2'-carboxy-diphenylsulfide derivative, and subjecting the obtained 2-amino-2'-carboxy-diphenylsulfide derivative to dehydration-condensation reaction.