1293489-87-8Relevant articles and documents
Photocatalytic Water-Splitting Coupled with Alkanol Oxidation for Selective N-alkylation Reactions over Carbon Nitride
Xu, Yangsen,Zhang, Zhaofei,Qiu, Chuntian,Chen, Shaoqin,Ling, Xiang,Su, Chenliang
, p. 582 - 589 (2021)
Photocatalytic water splitting technology (PWST) enables the direct use of water as appealing “liquid hydrogen source” for transfer hydrogenation reactions. Currently, the development of PWST-based transfer hydrogenations is still in an embryonic stage. Previous reports generally centered on the rational utilization of the in situ generated H-source (electrons) for hydrogenations, in which photogenerated holes were quenched by sacrificial reagents. Herein, the fully-utilization of the liquid H-source and holes during water splitting is presented for photo-reductive N-alkylation of nitro-aromatic compounds. In this integrate system, H-species in situ generated from water splitting were designed for nitroarenes reduction to produce amines, while alkanols were oxidized by holes for cascade alkylating of anilines as well as the generated secondary amines. More than 50 examples achieved with a broad range scope validate the universal applicability of this mild and sustainable coupling approach. The synthetic utility of this protocol was further demonstrated by the synthesis of existing pharmaceuticals via selective N-alkylation of amines. This strategy based on the sustainable water splitting technology highlights a significant and promising route for selective synthesis of valuable N-alkylated fine chemicals and pharmaceuticals from nitroarenes and amines with water and alkanols.
Novel process for preparation of 1-[2-(2,4-dimethylphenylsulphanyl)phenyl] piperazine
-
Paragraph 0010; 0012, (2016/12/07)
The present invention discloses a novel process for the preparation of 1-[2-(2,4-dimethylphenylsulphanyl)phenyl] piperazine. The process uses o-halogenated benzenesulfonic acid and m-xylene as raw materials, which are subjected to dehydration condensation with methylsulfonic acid and phosphorus pentoxide as condensing agents to generate halogenated diarylsulfone. Halogenated diarylsulfone and piperazine are subjected to a substitution reaction in an aprotic solvent to produce piperazine ring substituted diarylsulfone; the piperazine ring substituted diarylsulfone is reduced by hexachlorodisilane in an aprotic solvent to obtain a product with high yield. This method has the advantages of cheap and easily available raw materials, avoidance of the usage of a noble metal catalyst and treatment of residual palladium, simple operation, mild reaction conditions, simple post-treatment, and potential application values.
Novel method for preparing vortioxetine
-
Paragraph 0023, (2016/11/17)
The invention relates to a novel method for preparing vortioxetine. Reduction, nucleophilic substitution and coupling are conducted on a 2-nitroiodobenzene compound, and a compound of 1-[2-(2,4-dimethyl phenyl sulfanyl)-phenyl]methyl piperazine; then the obtained compound reacts with phenyl chloroformate to obtain 1-[2-(2,4-dimethyl phenyl sulfanyl)-phenyl]piperazine-1-carboxylic acid phenyl ester which generates vortioxetine after being hydrolyzed under the alkaline condition.
