53662-48-9

Upstream product

• 75-15-0 carbon disulfide 
• 121-44-8 triethylamine 
• 108-42-9 3-chloro-aniline 

Downstream Products

• 77959-40-1 4-m-chlorophenyl-5-phenylimino-3-thio-1,2,4-thiadiazolidine 
• 77959-45-6 5-thio-2-phenylimino-4-m-chlorophenyl-1,3,4-dithiazolidine 
• 1028-38-2 2-sulfhydryl-3-(3-chlorophenyl)-quinazolin-4(3H)-one 
• 1012124-64-9 2-[3-(3-chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-ylsulfanyl]-propionic acid methyl ester 
• 193826-31-2 [3-(3-chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-ylsulfanyl]-acetic acid methyl ester 
• 193826-39-0 [3-(3-chloro-phenyl)-4-oxo-3,4-dihydro-quinazolin-2-ylsulfanyl]-acetic acid hydrazide 
• 2392-68-9 3-chlorophenyl-isothiocyanate 
• 4947-89-1 1-(3-chlorophenyl)-2-thiourea 
• 54507-99-2 N-(3-chlorophenyl)cyanamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway

In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound 19e had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound 19e also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound 19e exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound 19e could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound 19e targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Molecular docking showed that compound 19e could bind into the active pocket of EGFR. Those work suggested that compound 19e would have remarkable implications for further design of anti-tumor agents.

Na2S2O8-mediated efficient synthesis of isothiocyanates from primary amines in water

We have developed two green, practical, and efficient procedures, including a one-pot one, to synthesize isothiocyanates from amines and carbon disulfide via desulfurization with sodium persulfate. Water is used as the solvent. Basic conditions are necessary for good chemoselectivity for isothiocyanates. Structurally diverse linear and branched alkyl amines and aryl amines are readily converted to isothiocyanates by the two procedures in satisfactory yields. Halogens, benzylic C-H bonds, methylthio, nitro, ester, alkenyl, electron-rich or -deficient (hetero)aryls, acetylenyl, and even phenolic and alcoholic hydroxyls are well tolerated. The one-pot procedure in water can also be used to realize the preparation of chiral isothiocyanates from chiral amines, and the modification of bioactive structures with free amino groups. In large-scale preparation, simple and practical purification procedures independent of column chromatography are developed.

Double three bromo 1,3-di-pyridine salt-based propane and its preparation method, method of use, recovery method and application

The invention discloses a double tribromo 1,3-bipyridine onium salt dimethylmethane, and a preparation method, an application method, a recovery method and application thereof. The preparation method comprises the following steps: dissolving 1,3-bipyridine onium salt dimethylmethane by using water, and then adding potassium bromide; adding potassium peroxymonosulfate sulfate compound brine solution to prepare a clear solution after dissolving potassium bromide, and then stirring and reacting at -10 to 0 DEG C until solid is separated out; separating out solid, so as to obtain the double tribromo 1,3-bipyridine onium salt dimethylmethane. The product can be used for preparing isothiocyanate, aromatic thiourea or acetanilide. The preparation method disclosed by the invention is mild in condition, and simple to operate the reaction process, and raw materials are easily available. The double tribromo 1,3-bipyridine onium salt dimethylmethane not only can be used as a brominating reagent, but also can be used as organic synthesis intermediates, meanwhile, the reaction efficiency is improved, and the double tribromo 1,3-bipyridine onium salt dimethylmethane is convenient to recover and can be recycled.

3,4-diarylthiazolin-2-one or -2-thione derivatives, their methods of preparation and their uses in their methods of preparation and their uses in therapeutics

The present invention relates to derivatives of formula STR1 and to their use in therapeutics especially as drugs with anti-inflammatory and analgesic properties.

New Heterocyclic Compounds : 5-Oxo/thio-4-aryl-2-phenylimino-1,3,4-dithiazolidines

5-Oxo/thio-4-aryl-2-phenylimino-1,3,4-dithiazolidines (VI and IX) have been prepared by reaction of S-chloro-N-phenylisothiocarbamoyl chloride and triethylamine salts of arylthiocarbamic acids and aryldithiocarbamic acids respectively.VI and IX when boiled with benzylamine give the same product (XI).The structures of all these products have been assigned on the basis of chemical transformations and IR data.Probable mechanisms of these reactions are also suggested.