423738-98-1

Upstream product

• 6285-57-0 2-amino-6-nitrobenzothiazole 
• 2131-61-5 p-nitrophenyl isothiocyanate 
• 110-91-8 morpholine 
• 4845-58-3 6-nitrobenzo[d]thiazole-2(3H)-thione 
• 149-30-4 2-thioxo-3H-1,3-benzothiazole 
• 137-07-5 2-amino-benzenethiol 
• 364339-83-3 N-(4-nitrophenyl)-N’-morpholinothiourea 
• 4845-58-3 2-mercapto-6-nitrobenzothiazole 
• 2407-11-6 2-chloro-6-nitrobenzothiazole 

Downstream Products

• 1400420-80-5 4-(6-(4-phenyl-1H-1,2,3-triazol-1-yl)benzo[d]thiazol-2-yl)morpholine 
• 850021-27-1 2-morpholinobenzo[d]thiazol-6-amine 

Relevant academic research and scientific papers

A Mild Synthesis of 2-Substituted Benzothiazoles via Nickel-Catalyzed Intramolecular Oxidative C-H Functionalization

A highly efficient synthetic method for the preparation of 2-aminobenzothiazoles starting from arylthioureas has been reported. By using a nickel catalyst, arylthioureas undergo intramolecular oxidative C-H bond functionalization, giving the desired 2-aminobenzothiazoles in good to excellent yields. This protocol features an inexpensive catalyst, low catalyst loading, mild reaction conditions, a short reaction time, and good to excellent yields, and it can be scaled up easily to a gram scale with almost no yields decreasing.

Ruthenium catalyzed intramolecular C-S coupling reactions: Synthetic scope and mechanistic insight

A ruthenium catalyzed intramolecular C-S coupling reaction of N-arylthioureas for the synthesis of 2-aminobenzothiazoles has been developed. Kinetic, isotope labeling, and computational studies reveal the involvement of an electrophilic ruthenation pathwa

Eosin y catalyzed visible-light-promoted aerobic oxidative cyclization of 2-aminobenzothiazole

A mild and efficient one-pot visible light irradiated synthesis of 2-aminobenzothiazole 4(a-l) from arylisothiocyanate 1(a-l) and secondary amines 2 have been reported in presence of eosin Y as an organophotoredox catalyst at room temperature under aerobi

Gold nanoparticle catalyzed intramolecular C-S bond formation/C-H bond functionalization/cyclization cascades

An efficient synthesis of 2-(N-aryl)aminobenzo[d]-1,3-thiazoles via intramolecular C-S bond formation/C-H bond functionalization utilizing an unusual cocatalytic Au-NPs/KMnO4 system under an oxygen atmosphere at 80 °C is presented. Au-NPs can b

Arylation of amines and monoarylation of symmetrical diamines in the presence of brine solution with diheteroaryl halides

A simple, scalable, ligand-free, and metal-free protocol for arylation of amines and monoarylation of symmetrical diamines with diheteroaryl halides in the presence of brine solution has been developed. The protocol has broad structural applicability for chemoselective monoarylation of a wide variety of symmetrical, cyclic, and acyclic aliphatic diamines. The protocol is also applicable for selective arylation of aliphatic amine in the presence of aromatic amine.

BICYCLIC HETEROCYCLES AS IRAK4 INHIBITORS

The present invention provides bicyclic heterocycle kinase enzyme inhibitor compounds of formula (I), which may be therapeutically useful as kinase inhibitor, more particularly IRAK4 inhibitors. ( I ) in which A, R, R1,R2, m, n and p have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting kinase enzyme, more particularly IRAK4 enzyme.The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

A DBU-diheteroaryl halide adduct as the fastest current N-diheteroarylating agent

An unexpected diazabicyclo[5.4.0]undec-7-ene (DBU) catalysed rate enhancement of N-arylation of amines with diheteroaryl halides is reported. DBU is found to activate the Ar-Cl bond of a diheteroaryl halide, forming a green coloured adduct under neat conditions. The activated green coloured adduct was used for the arylation of amines under neat conditions and was found to be the fastest diheteroarylating agent reported to date. The Royal Society of Chemistry 2013.

Triazolbenzo[d]thiazoles: Efficient synthesis and biological evaluation as neuroprotective agents

A number of (1H-1,2,3-triazol-1-yl)benzo[d]thiazoles were synthesized utilizing a versatile Cu-catalyzed azide-alkyne click reaction (CuAAC) on tautomeric benzo[4,5]thiazolo[3,2-d]tetrazole (1) and 2-azidobenzo[d]thiazole (2) starting materials. Moreover, one of the resulting products of this investigation, triazolbenzo[d]thiazole 22, was found to possess significant neuroprotective activity in human neuroblastoma (SH-SY5Y) cells.

Chemospecific and ligand free CuI catalysed heterogeneous N-arylation of amines with diheteroaryl halides at room temperature

A ligand free, copper-catalyzed N-arylation reaction of amines with diheteroaryl halides in heterogeneous medium at room temperature has been developed. The protocol is very effective for low boiling amines and useful for amines available in aqueous solution. The reaction gives chemospecific arylation of amines with diheteroaryl halides in the mixture monoheteroaryl halides, diheteroaryl halides and carbocyclic aryl halides. The reaction is also chemospecific with respect to arylation of aliphatic amines. Monoarylated piperazines were also synthesized at room temperature following this protocol. The Royal Society of Chemistry 2011.

Heterocycle formation via palladium-catalyzed intramolecular oxidative C-H bond functionalization: An efficient strategy for the synthesis of 2-aminobenzothiazoles

N-Arylthioureas are converted to 2-aminobenzothiazoles via Intramolecular C-S bond formation/C-H functionalization utilizing an unusual cocatalytic Pd(PPh3)4MnO2 system under an oxygen atmosphere at 80 °C. This method elim