22868-34-4Relevant articles and documents
A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain
Mathis, Chester A.,Bacskai, Brian J.,Kajdasz, Stephen T.,McLellan, Megan E.,Frosch, Matthew P.,Hyman, Bradley T.,Holt, Daniel P.,Wang, Yanming,Huang, Guo-Feng,Debnath, Manik L.,Klunk, William E.
, p. 295 - 298 (2002)
The synthesis of a new lipophilic thioflavin-T analogue (2-[4′-(methylamino)phenyl]benzothiazole, 6) with high affinity for amyloid is reported. Intravenous injection of [11C]-labeled 6 in control mice resulted in high brain uptake. Amyloid dep
Iodine-catalyzed, one-pot, solid-phase synthesis of benzothiazole derivatives
Gupta, Sayan Dutta,Singh, Hemendra Pratap,Moorthy
, p. 4327 - 4329 (2007)
Molecular iodine was utilized in a one-pot, solid-phase, solvent-free reaction between 2-aminothiophenol and benzoic acid derivatives to obtain highly economical and excellent yield of benzothiazole derivatives in comparison to polyphosphoric acid- and [pmIm]-Br-catalyzed microwave synthesis reactions. The results of the studies revealed that the new method reduces cost by approximately 17-fold in comparison to polyphosphoric acid and has a significant cost reduction in comparison to [pmIm]-Br. Moreover, it becomes even more economical because no additional chemicals and solvents are necessary for the reaction. Copyright Taylor & Francis Group, LLC.
Method for catalyzing nitrogen heterocyclic ring aerobic dehydrogenation based on ionic liquid porous carbon material
-
Paragraph 0040-0043, (2022/01/24)
The invention discloses a method for catalyzing nitrogen heterocycle aerobic dehydrogenation based on an ionic liquid porous carbon material, and is suitable for the field of organic synthesis. A heterogeneous catalysis system takes nitrogen heterocycle and derivatives thereof as substrates, a carbon material as a catalyst, water or ethanol as a solvent and air or oxygen spheres as an oxygen source, and a reaction is carried out at 0-80 DEG C under normal pressure, oxidative dehydrogenation of nitrogen heterocyclic compounds can be realized, and target products such as indole, quinoline, isoquinoline, quinazoline, quinoxaline, benzothiazole, Hanus ester and derivatives thereof and other medical intermediates can be synthesized. The non-metal catalyst is prepared by using the ionic liquid as the precursor, no activating agent or other additives are used in the reaction process, and the method has industrial application prospects.
Method for catalytically synthesizing benzothiazole compound by using copper complex
-
Paragraph 0056-0067, (2021/09/22)
The invention relates to a method for catalytically synthesizing benzothiazole compounds by using a copper complex, which is characterized in that a copper complex containing ortho-carborane Schiff base ligand is used as a catalyst to form aldehydes. 2 - Bromoaniline and sodium sulfide are used as raw materials, and the reaction is carried out at room temperature to obtain a benzothiazole compound. Compared with the prior art, the copper complex catalytic aldehyde, 2 -bromoaniline and sodium sulfide (Na) containing the ortho-carborane Schiff base ligand are utilized. 2 Multiple components of S) react to prepare benzothiazole compounds, and the catalyst is low in dosage, mild in reaction conditions, high in reaction rate, high in yield, wide in substrate range, cheap and accessible in raw materials and wide in application prospect in industry.
Novel series of benzo[d]thiazolyl substituted-2-quinolone hybrids: Design, synthesis, biological evaluation and in-silico insights
Bolakatti, Girish,Palkar, Mahesh,Katagi, Manjunatha,Hampannavar, Girish,Karpoormath, Rajshekhar V.,Ninganagouda, Shilpa,Badiger, Arvind
, (2020/10/30)
A novel series of 3-(2-(4-(substituted-benzo[d]thiazol-2-yl)phenylamino)acetyl)-4?hydroxy-1-methyl/phenyl quinolin-2(1H)-one (7a-f and 8a-f) were synthesized. Reaction of appropriately substituted-2-(4-amino phenyl)benzo[d]thiazole (4a-f) with 3-(2-bromoacetyl)-4?hydroxy-1-methyl/phenyl quinolin-2(1H)-one (5/6) in the presence of glacial acetic acid resulted in desired compounds. Structures of the synthesized compounds were characterized based on their spectral (IR, 1H NMR, 13C NMR and MS) and elemental analysis. The cytotoxicity screening studies revealed that MCF-7 and WRL68 cancer cells were sensitive to all the tested compounds. Out of twelve novel hybrids, compound 8f displayed the most significant anticancer activity. Docking studies were performed in order to understand the binding mode of the title compounds at the active site of the target enzyme (EGFR tyrosine kinase, 1M17). Compounds 8f and 7f displayed prominent and conserved binding interactions against 1M17. In addition, compounds 7e, 7f, 8e, and 8f exhibited interesting in vitro antibacterial activity, especially against Gram-negative bacteria E. coli. In summary, the novel benzo[d]thiazolyl substituted-2-quinolone hybrid (8f) could be considered as promising hit and could be further exploited for developing potential anticancer/antimicrobial agents.