804549-56-2

Upstream product

• 32137-73-8 2-(trimethylsilyl)benzothiazole 
• 1711-06-4 3-Methylbenzoyl chloride 
• 72927-80-1 (3-methylphenyl)acetaldehyde 
• 137-07-5 2-amino-benzenethiol 
• 100-80-1 3-methylstyrene 
• 143278-20-0 2-iodo-1-(3-methylphenyl)ethanone 
• 95-16-9 1,3-Benzothiazole 
• 108-38-3 m-xylene 
• 944655-40-7 (benzothiazol-2-yl)(m-tolyl)methanol 
• 97065-56-0 1-(2,2-dibromovinyl)-3-methylbenzene 
• 33675-43-3 1-(bromo-ethynyl)-3-methyl-benzene 
• 585-74-0 3-Methylacetophenone 

Downstream Products

• 1256158-37-8 bis(1,3-benzothiazol-2-yl)(3-methylphenyl)methanol 
• 1370436-43-3 [(benzothiazol-2-yl)(m-tolyl)methylene](1-methylpiperidin-4-yl)amine 

Relevant academic research and scientific papers

Photoinduced remote heteroaryl migration accompanied by cyanoalkylacylation in continuous flow

A photoinduced 1,4-heteroaryl migration from a carbon center to a nitrogen center accompanied by a cyanoalkylacylation of heterocyclic-substituted azidyl homoallylic alcohols and cycloketone oxime esters has been described. This simple and powerful protoc

C2 substituted 2H-benzothiazole aryl acylated derivative, and synthesis method and application thereof

The invention discloses a C2 substituted 2H-benzothiazole aryl acylated derivative, and a synthesis method and application thereof. The preparation method of the derivative comprises the following steps: mixing substituted 2H-benzothiazole and substituted methyl benzene, adding into a solvent, in the presence of an oxidizing agent Selectfluor and an additive trifluoroacetic acid, carrying out a heating and stirring reaction in the air atmosphere, performing TLC monitoring is conducted till the reaction is finished, and separating and purifying the obtained reaction liquid to obtain the target product C2 substituted 2H-benzothiazole aryl acylated derivative. The substituted methyl benzene used in the invention is low in price, easy to obtain and good in chemical stability, the method has the advantages of being high in atom economy, simple in catalytic system, free of transition metal catalysts, good in product yield, wide in substrate range and the like, and the prepared compound structure can be further optimized as an anti-tumor drug lead.

C2-arylacylation of 2H-benzothiazoles with methyl arenes via Selectfluor oxidation

An efficient Selectfluor-oxidative protocol was developed for the direct C2-arylacylation of 2H-benzothiazoles via the radical reaction of 2H-benzothiazoles with methyl arenes. Selectfluor can effectively promote the oxidative cross-coupling without an ex

Iodine- And TBHP-Promoted Acylation of Benzothiazoles under Metal-Free Conditions

A simple protocol for the synthesis of 2-acylbenzothiazoles using aryl ketones and benzothiazoles in the presence of I 2and TBHP is described. Acylation of the benzothiazoles is achieved through a sequence involving oxidation of the aryl ketone to an aryl glyoxal, ring-opening of the benzothiazole followed by condensation of the amino group with the aryl glyoxal, cyclization and oxidation. The method avoids the use of metals and toxic solvents. In addition, this protocol has the advantage of broad scope and provides good to excellent product yields.

Chemoselective copper-catalyzed acylation of benzothiazoles with aryl methyl ketones

A copper(I) iodide-catalyzed, highly efficient acylation of benzothiazoles with aryl methyl ketones as carbonyl sources under a nitrogen atmosphere was developed. This is an unprecedented protocol and an extremely efficient method for the selective synthesis of 2-acylbenzothiazoles from commercially available, cheap starting materials with excellent chemoselectivity, good functional group tolerability and high turnover numbers (up to 14,200); also scaling up to 160mmol without loss of the efficiency is possible. A variety of 2-acylbenzothiazoles was smoothly prepared in good to excellent yields from aryl methyl ketones and benzothiazoles by a one-pot domino protocol of combined sp3 C-H oxidation, ring opening, and condensation.

A multipathway coupled domino strategy: Metal-free oxidative cyclization for one-pot synthesis of 2-acylbenzothiazoles from multiform substrates

A multipathway coupled domino strategy has been developed for the efficient synthesis of 2-acylbenzothiazoles from multiform substrates arylethenes, arylacetylenes, 2-hydroxy-aromatic ketones, and carbinols via four distinct pathways. Through a logical coupled oxidation/heterocyclization domino process, a variety of 2-acylbenzothiazoles were synthesized free of metal in one pot.

BENZAZOLE DERIVATIVES AS HISTAMINE H4 RECEPTOR LIGANDS

The present patent application concerns new Iigands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.

Benzazole derivatives as histamine H4 receptor ligands

The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.

Rucl33h2o catalyzed tandem reaction of alkynylbromides with 2-aminothiophenols in water: A convenient synthesis of 2-benzoylbenzothiazoles

RuCl33H2O catalyzed tandem reaction of alkynyl bromides with 2-aminothiophenols mediated by water is shown to represent a convenient synthesis of 2-benzoylbenzothiazoles. In addition, the Ru(iii) catalyst could be readily recovered and efficiently reused together with water up to three times. CSIRO 2011.

Synthesis of heteroaryl ketones via tandem reaction of 1,1-dibromoethenes

A novel method for the synthesis of heteroaryl ketones through one-pot tandem reaction of 1,1-dibromoethenes with 2-amino(thio)phenols promoted by TBAF·3H2O and RuCl3(5%)/air was developed. This novel method includes several reactions in one-pot and utilizes economical yet efficient reagents to generate synthetically and biologically interesting heteroaryl ketones under mild conditions with good efficiency.