9/23 News Final Thoughts on Chemistry for 2-Bromobenzothiazole

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A novel series of imidazoisoindoles were identified as potent indoleamine-2,3-dioxygenase (IDO) inhibitors. Lead optimization toward improving potency and eliminating CYP inhibition resulted in the discovery of lead compound 25, a highly potent IDO inhibitor with favorable pharmacokinetic properties. In the MC38 xenograft model in hPD-1 transgenic mice, 25 in combination with the anti-PD-1 monoclonal antibody (SHR-1210) achieved a synergistic antitumor effect superior to each single agent.

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Thiazole | C3H2751NS – PubChem,
Thiazole | chemical compound | Britannica

23-Sep News Simple exploration of 2-Bromobenzothiazole

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The present invention refers to heterocyclic substituted 2 – it will be biting, this phenyl imidazo [1, 2 -a] Pyridine derivatives, and manufacturing method of the active ingredient for the prevention or treatment of diseases associated to pharmaceutical compositions including GLP-a 1 receptor activity are disclosed. The present invention according to it will be biting, this substituted 2 – heterocyclic phenyl imidazo [1, 2 -a] Pyridine derivatives (Glucagon a-like peptide 1 Receptor) so that the ability to activate GLP-a 1 receptor, can be useful analogs of GLP-a 1, diseases associated with GLP-a 1 receptor activity, specifically can be used in the treatment of metabolic syndrome, in particular, can be useful in preventing or treating obesity or diabetes. (by machine translation)

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Thiazole | C3H2654NS – PubChem,
Thiazole | chemical compound | Britannica

9/23/21 News A new application about 2-Bromobenzothiazole

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A CuCl-catalyzed Ullmann-type C-N cross-coupling reaction of carbazoles and 2-bromopyridine derivatives has been developed for the synthesis of N-heteroarylcarbazole derivatives employing 1-methyl-imidazole and t-BuOLi as ligand and base, respectively, both of which are found to significantly promote the reaction. Low cost and low loading of both catalyst and ligand, together with high reaction yields, render this practical reaction to be suitable for large-scale preparations and could be useful in material science.

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Reference:
Thiazole | C3H2757NS – PubChem,
Thiazole | chemical compound | Britannica

22-Sep News The important role of 2-Bromobenzothiazole

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Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

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Thiazole | C3H2718NS – PubChem,
Thiazole | chemical compound | Britannica

Sep 2021 News Discovery of 2-Bromobenzothiazole

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A novel and convergent palladium catalyzed synthesis of 2-arylbenzothiazoles has been investigated. The key step in the synthesis is a Suzuki biaryl coupling of 2-bromobenzothiazole with aryl boronic acids to provide a variety of 2-arylbenzothiazole derivatives in good yield. The synthetic utility of this methodology is demonstrated by the synthesis of 2-(4-aminophenyl)-6-methoxybenzothiazole, a PET probe precursor for the in vivo imaging of Alzheimer’s disease.

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Reference:
Thiazole | C3H2752NS – PubChem,
Thiazole | chemical compound | Britannica

08/9/2021 News The Absolute Best Science Experiment for 2-Bromobenzothiazole

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Biological thiols play important roles in maintaining appropriate redox status of organisms. Accepting the challenge to differentiate structurally similar cysteine (Cys) and homocysteine (Hcy), we have successfully developed a miniature synthetic turn-on fluorescent probe based on 6-(2-benzothiazolyl)-2-naphthalenol for Cys. This probe is able to specifically react with Cys to yield its naphthalenol derivative, accompanied by remarkable green fluorescence enhancement with a detection limit of 14.8 nM. Besides, this probe displays much greater selectivity for Cys over other biological thiols, including homocysteine (Hcy) and glutathione (GSH). Practically, good cell permeability and low cytotoxicity make it suitable for monitoring basal Cys in living cells.

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Thiazole | C3H2728NS – PubChem,
Thiazole | chemical compound | Britannica

The important role of 2-Bromobenzothiazole

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Herein, we report a convenient and broadly applicable strategy for the difluoromethylation of aryl bromides by metallaphotoredox catalysis. Bromodifluoromethane, a simple and commercially available alkyl halide, is harnessed as an effective source of difluoromethyl radical by silyl-radical-mediated halogen abstraction. The merger of this fluoroalkyl electrophile activation pathway with a dual nickel/photoredox catalytic platform enables the difluoromethylation of a diverse array of aryl and heteroaryl bromides under mild conditions. The utility of this procedure is showcased in the late-stage functionalization of several drug analogues.

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Reference:
Thiazole | C3H2705NS – PubChem,
Thiazole | chemical compound | Britannica

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The present invention has offered a kind of ortho-carborane benzothiazole structure of semi-[…] complex and its preparation. The invention relates to a compound […] [Cp * IrCl2 ]2 As the raw material, it is connected to the n – BuLi, ortho-carborane benzothiazole reaction, to obtain ortho-carborane benzothiazole […] complex structure, the invention synthesis technique is simple green, has excellent selectivity and high yield. The invention iridium complex has stable physical and chemical properties and characteristics such as thermal stability, and under the condition of MAO as cocatalyst can be under the normal pressure effectively catalyze polymerization of ethylene, the obtained polymer also has relatively high molecular weight. (by machine translation)

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Reference:
Thiazole | C3H2660NS – PubChem,
Thiazole | chemical compound | Britannica

Final Thoughts on Chemistry for 2-Bromobenzothiazole

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A simple and efficient protocol for the copper-catalyzed synthesis of aryl or alkyl 2,2,2-trifluoroethyl selenoethers has been developed. This reaction proceeded smoothly in the presence of CuI/phen as the catalyst, with elemental selenium, 1,1,1-trifluoro-2-iodoethane, and NaBH4 as reagents in DMF with a broad scope of functionalized (hetero)aryl or alkyl halides. Different functional groups were tolerated and moderate to excellent yields of 2,2,2-trifluoroethyl selenoethers were obtained. Some of the synthesized compounds exhibited promising insecticidal activities.

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Reference:
Thiazole | C3H2743NS – PubChem,
Thiazole | chemical compound | Britannica

The important role of 2-Bromobenzothiazole

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Our development of PDE10A inhibitors began with an HTS screening hit (1) that exhibited both high p-glycoprotein (P-gp) efflux ratios in rat and human and poor metabolic stability. On the basis of cocrystal structure of 1 in human PDE10A enzyme, we designed a novel keto-benzimidazole 26 with comparable PDE10A potency devoid of efflux liabilities. On target in vivo coverage of PDE10A in rat brain was assessed using our previously reported LC-MS/MS receptor occupancy (RO) technology. Compound 26 achieved 55% RO of PDE10A at 30 mg/kg po and covered PDE10A receptors in rat brain in a dose-dependent manner. Cocrystal structure of 26 in PDE10A confirmed the binding mode of the novel scaffold. Further optimization resulted in the identification of keto-benzimidazole 34, which showed an increased in vivo efficacy of 57% RO in rats at 10 mg/kg po and an improved in vivo rat clearance and oral bioavailability.

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Thiazole | C3H2693NS – PubChem,
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