2544-92-5

Upstream product

• 46055-91-8 2-benzothiazol-2-yl-ethanol 
• 615-20-3 2-chlorobenzo[d][1,3]thiazole 
• 6639-57-2 benzothiazole-2-carbaldehyde 
• 2065-66-9 methyl-triphenylphosphonium iodide 
• 120-75-2 2-Methylbenzothiazole 
• 50-00-0 formaldehyd 
• 615-22-5 2-methylmercaptobenzothiazole 
• 7486-35-3 tri-n-butyl(vinyl)tin 
• 137-07-5 2-amino-benzenethiol 
• 625-36-5 2-chloropropionyl chloride 

Downstream Products

• 88611-57-8 5-benzothiazol-2-yl-pentan-2-one 
• 41387-91-1 4-(2-Benzothiazolyl)butansaeure 
• 20614-71-5 2-pentylbenzo[d]thiazole 

Relevant academic research and scientific papers

Nickel(ii)-catalyzed addition of aryl-, alkenyl-, and alkylboronic acids to alkenylazaarenes

A nickel(II)-catalyzed addition of aryl-, alkenyl-, and alkylboronic acids to alkenylazaarenes was presented. This reaction exhibited high efficiency (up to 93% yield), a broad substrate scope (seven types of heterocycles), and good functional group compatibility. The resulting products can be further transformed to many useful building blocks. Finally, the preliminary studies suggested that the adjacent N atom of the heterocycles was essential for the high reactivity.

Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening

The histone acetyltransferases (HATs) in mammals include GCN5 N-acetyltransferases, the MOZ, YBF2, SAS2, and TIP60 proteins, and the orphan HATs. The males absent on the first (MOF) is mainly related to acetylation of histone H4 Lys16 and has influence on downstream genes expression. However, the only inhibitor MG149 presented low activity against MOF. Besides, there was no high throughput screening platform on MOF, which limited the inhibitor discovery and functional study. In our study, we set up a high throughput screening platform based on amplified luminescent proximity homogeneous assay (ALPHA), which led us to a moderate inhibitor DC_M01. By chemical modification, we found DC_M01_7, which was the analog of DC_M01 with an IC50 value of 6 μM. DC_M01_7 significantly inhibited HCT116 cells proliferation and could also inhibit histone 4 lysine 16 acetylation in HCT116 cells. To sum up, our work will probably assist the further development of more potent MOF inhibitors and the functional study of hMOF.

Copper-catalyzed borylative coupling of vinylazaarenes and N-Boc imines

Cu-catalyzed three-component couplings of vinylazaarenes, B2(pin)2, and N-Boc imines are described. Oxidation of the initially formed boronate gives azaarene-containing, Boc-protected amino alcohols with reasonable to good diastereoselectivities.

Facile catalyst-free synthesis of 2-vinylquinolines via a direct deamination reaction occurring during Mannich synthesis

A facile catalyst-free method for the synthesis of 2-vinylquinolines via a direct deamination reaction during Mannich synthesis has been developed. Instantaneous hydrogen transfer via a six-membered ring intermediate is proposed as a key step for the direct deamination reaction. This reaction strategy tolerates a broad substrate scope and provides a highly efficient way to synthesize 2-vinylquinolines with adequate yields.

Enantioselective copper-catalyzed reductive coupling of vinylazaarenes with n -boc aldimines

The diastereo- and enantioselective reductive coupling of vinylazaarenes with N-Boc aldimines is described. The reactions proceed using chiral copper-bisphosphine complexes in the presence of TMDS as a hydride source to give reductive coupling products in moderate to high enantioselectivities.

Copper(I)-promoted palladium-catalyzed cross-coupling of unsaturated tri-n-butylstannane with heteroaromatic thioether

(Matrix presented) Palladium-catalyzed cross-coupling of vinyl- and arylstannanes with π-electron-deficient heteroaromatics was performed in good yields. This Stille-type reaction was carried out with a methylthioether function as an electrophile in the presence of a copper(I) bromide-dimethyl sulfide complex.