91813-44-4

Upstream product

• 936-61-8 Thiobenzoic acid O-ethyl ester 
• 20511-15-3 3-amino-4-chloropyridine 
• 59171-46-9 N-(3-pyridinyl)phenylthioamide 
• 17452-27-6 pyridin-3-yl isothiocyanate 
• 273-75-6 thiazolo[4,5-c]pyridine 
• 591-50-4 iodobenzene 
• 89002-13-1 3-amino-4-mercaptopyridine 
• 462-08-8 pyridin-3-ylamine 
• 100-52-7 benzaldehyde 
• 5221-40-9 N-(3-pyridinyl)benzamide 

Relevant academic research and scientific papers

Kinase inhibitor, and preparation and application of kinase inhibitor

The invention provides a compound shown as a formula (I), or a stereoisomer, a tautomer, nitrogen oxide, metabolite, a prodrug, pharmaceutically acceptable salt or solvate of the compound, and application of the compound to preparing drugs or drug compositions for treating Pim kinase-mediated diseases.

Catalyst- and Supporting-Electrolyte-Free Electrosynthesis of Benzothiazoles and Thiazolopyridines in Continuous Flow

A catalyst- and supporting electrolyte-free method for electrochemical dehydrogenative C?S bond formation in continuous flow has been developed. A broad range of N-arylthioamides have been converted to the corresponding benzothiazoles in good to excellent yields and with high current efficiencies. This transformation is achieved using only electricity and laboratory grade solvent, avoiding degassing or the use of inert atmosphere. This work highlights three advantages of electrochemistry in flow, which is (i) a supporting electrolyte-free reaction, (ii) an easy scale-up of the reaction without the need for a larger reactor and, (iii) the important and effective impact of having a good mixing of the reaction mixture, which can be achieved effectively with the use of flow systems. This clearly improves the reported methods for the synthesis of benzothiazoles.

Palladium-catalyzed C-H cyclization in water: A milder route to 2-arylbenzothiazoles

Water was successfully employed as a reaction medium in palladium-catalyzed C-H cyclization of thiobenzanilides. Reactions efficiently proceeded under considerably mild conditions such as 40 °C in water, providing a more practical, greener method for the synthesis of 2-arylbenzothiazoles. For some substrates, the addition of an amphiphilic surfactant greatly enhanced the process. The method represents a rare example of palladium-catalyzed C-H functionalization processes performed in water. Georg Thieme Verlag Stuttgart · New York.

Use of molecular oxygen as a reoxidant in the synthesis of 2-substituted benzothiazoles via palladium-catalyzed C-H functionalization/intramolecular C-S bond formation

Molecular oxygen (O2) was successfully employed as a reoxidant in cyclizations of thiobenzanilides 1a-s through a palladium-catalyzed C-H functionalization/intramolecular C-S bond formation process, leading to an efficient, green method for the synthesis of 2-arylbenzothiazoles 2a-s. Addition of cesium fluoride (CsF) greatly enhanced the reactions, which produced variously substituted 2-arylbenzothiazoles with good functional group tolerance. Thioureas 4a-j were also found to be suitable substrates for the cyclization process using a palladium/O2 catalyst system, thus generating 2-aminobenzothiazoles 5a-j. One-pot syntheses of 2-aminobenzothiazoles 5a-j from aryl isothiocyanates 6 and amines 7 were also successful.

Nouvelle methode de synthese de thiazolopyridines

It has been established that the direct condensation between aromatic and aliphatic thioesters and the variously generated anion of aminochloropyridines represents the best method for the synthesis of thiazolopyridines.The transient thioamides, sometimes isolated, can be easily converted chemically or photochemically into the desired fused heterocycles.

2-ARYL-OXAZOLO- AND THIAZOLOPYRIDINES. SYNTHESIS VIA CYCLIZATION OF N-(2-CHLORO-3-PYRIDINYL)ARYLAMIDES AND THIOAMIDES

Chloropyridinylenamides can by easily converted into oxazolo- and thiazolo pyridines by treatment with polyphosphoric acid and Lawesson reagent respectively.