Category: 468075-00-5

Cox, Jason M. published the artcileDesign, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists, Recommanded Product: 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, the main research area is preparation GPR120 spirocyclic agonist diabetes; FFAR4; GPR120; insulin sensitization; spirocyclic; type 2 diabetes.

Type 2 diabetes mellitus (T2DM) is an ever increasing worldwide epidemic, and the identification of safe and effective insulin sensitizers, absent of weight gain, has been a long-standing goal of diabetes research. G-protein coupled receptor 120 (GPR120) has recently emerged as a potential therapeutic target for treating T2DM. Natural occurring, and more recently, synthetic agonists have been associated with insulin sensitizing, anti-inflammatory, and fat metabolism effects. Herein we describe the design, synthesis, and evaluation of a novel spirocyclic GPR120 agonist series, which culminated in the discovery of potent and selective agonist 14. Furthermore, compound 14 was evaluated in vivo and demonstrated acute glucose lowering in an oral glucose tolerance test (oGTT), as well as improvements in homeostatic measurement assessment of insulin resistance (HOMA-IR; a surrogate marker for insulin sensitization) and an increase in glucose infusion rate (GIR) during a hyperinsulinemic euglycemic clamp in diet-induced obese (DIO) mice.

ACS Medicinal Chemistry Letters published new progress about Antidiabetic agents. 468075-00-5 belongs to class chlorides-buliding-blocks, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, and the molecular formula is C7H3BrClF3O, Recommanded Product: 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Rombouts, Frederik J. R. published the artcilePyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors, Category: chlorides-buliding-blocks, the main research area is pyrido triazolo pyrazine brain phosphodiesterase inhibitor; PDE2 inhibitor; Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine; phosphodiesterase 2 inhibitor; selective; tricycle.

A novel series of pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines is reported as potent PDE2/PDE10 inhibitors with drug-like properties. Selectivity for PDE2 was obtained by introducing a linear, lipophilic moiety on the meta-position of the Ph ring pending from the triazole. The SAR and protein flexibility were explored with free energy perturbation calculations Rat pharmacokinetic data and in vivo receptor occupancy data are given for two representative compounds 6 and 12.

ACS Medicinal Chemistry Letters published new progress about Drug bioavailability. 468075-00-5 belongs to class chlorides-buliding-blocks, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, and the molecular formula is C7H3BrClF3O, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lachance, Nicolas published the artcileDiscovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series, COA of Formula: C7H3BrClF3O, the main research area is arylheterocyclyl thiazolyltetrazoleacetic thiadiazolyltetrazoleacetic acid preparation stearoyl CoA desaturase inhibitor; arylpyrrolopyrrole isoxazolyltetrazoleacetic acid preparation stearoyl CoA desaturase inhibitor; structure arylheterocyclyl thiazolyltetrazoleacetic thiadiazolyltetrazoleacetic acid inhibition stearoyl CoA desaturase; liver selectivity pharmacokinetics thiazolyltetrazoleacetic thiadiazolyltetrazoleacetic acid stearoyl desaturase inhibitor; tissue distribution stearoyl CoA desaturase inhibitor oral administration.

Arylheterocyclyl-substituted thiazolyltetrazoleacetic acids such as I and an isoxazolyltetrazoleacetic acid and a thiadiazolyltetrazoleacetic acid are prepared as inhibitors of stearoyl-CoA desaturase (SCD) with selectivity for the liver over other organs such as the skin and eyes in which SCD inhibitors cause undesired side effects. Coupling of a mono-Boc-protected perhydropyrrolopyrrole with 2-bromo-1-chloro-4-trifluoromethoxybenzene followed by Boc deprotection yielded a salt of the arylperhydropyrrolopyrrole II (either a chloride or trifluoroacetate); amidation of Et 2-bromo-5-thiazolecarboxylate, dehydration to the nitrile, and reaction with sodium azide yielded the bromothiazolyltetrazole III. Regioselective alkylation of III with a bromoacetate ester, coupling to II, and cleavage of the ester yielded I. The inhibition of stearoyl-CoA desaturase and its inhibition in rat hepatic cells and rat cells possessing active transporters by arylheterocyclyl-substituted thiazolyltetrazoleacetic acids and thiadiazolyltetrazoleacetic acids was determined; for I and two related compounds, their tissue distributions and in vivo stearoyl-CoA desaturase inhibitions on oral administration to mice were determined

Bioorganic & Medicinal Chemistry Letters published new progress about Active biological transport. 468075-00-5 belongs to class chlorides-buliding-blocks, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, and the molecular formula is C7H3BrClF3O, COA of Formula: C7H3BrClF3O.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Tsvelikhovsky, Dmitry published the artcileConcise Palladium-Catalyzed Synthesis of Dibenzodiazepines and Structural Analogues, COA of Formula: C7H3BrClF3O, the main research area is dibenzodiazepine dibenzooxazepine preparation palladium copper catalyzed cross coupling; aniline dihaloarene reactant palladium catalyzed coupling diarylamine preparation; diarylamine reactant palladium catalyzed cross coupling dibenzodiazepine preparation; phenol dihaloarene reactant palladium catalyzed coupling diarylether preparation; diarylether reactant palladium catalyzed cross coupling dibenzodiazepine preparation.

A general and highly efficient protocol for the synthesis of dibenzodiazepines and their structural analogs is reported. In the presence of catalytic quantities of palladium, readily accessible precursors are cross-coupled with ammonia and then spontaneously undergo an intramol. condensation to form the corresponding dibenzodiazepines, e.g. I, in one step. This new strategy is applicable to the construction of a wide variety of dibenzooxazepines, e.g. II, and other structurally related heterocycles, e.g. III.

Journal of the American Chemical Society published new progress about Aromatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 468075-00-5 belongs to class chlorides-buliding-blocks, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, and the molecular formula is C7H3BrClF3O, COA of Formula: C7H3BrClF3O.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Huang, Hai-Yun published the artcilePd-Catalyzed Direct Arylations of Heteroarenes with Polyfluoroalkoxy-Substituted Bromobenzenes, COA of Formula: C7H3BrClF3O, the main research area is fluoroalkoxy bromobenzene heteroarene palladium catalyst arylation; arylated heteroarene preparation.

The reactivity of di-, tri- and tetra-fluoroalkoxy-substituted bromobenzenes in the direct arylation of 5-membered ring heteroarenes using palladium catalysis was explored. High yields in arylated heteroarenes, e.g., I, were obtained using only 1 mol-% of Pd(OAc)2 catalyst with KOAc as an inexpensive base. Similar yields were obtained with o/m/p trifluoromethoxy-, o/p difluoromethoxy-, and tetrafluoroethoxy-substituents on the aryl bromide. A bromo-substituted difluorobenzo[d][1,3]dioxole was successfully coupled. The major side-products of the reaction are HBr/KOAc. Therefore, this synthetic scheme is very attractive for the access to such polyfluoroalkoxy-containing arylated heteroaromatics in terms of cost, simplicity, and low environmental impact, compared to reactions involving arylation of heteroarenes with bromophenols followed by polyfluoroalkylation.

European Journal of Organic Chemistry published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent) (fluoroalkoxy). 468075-00-5 belongs to class chlorides-buliding-blocks, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, and the molecular formula is C7H3BrClF3O, COA of Formula: C7H3BrClF3O.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

These common heterocyclic compound, 468075-00-5, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Safety of 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene

Into a two-dram vial was added-2-bromo-1-chloro-4-(trifluoromethoxy)benzene (100 mg, 0.363 mmol), the title compounds from Example 3 Step B (100 mg), and SPhos biaryi precatalysis (26.2 mg, 0.036 mmol), cesium carbonate (237 mg. 0.726 mmol) followed by 1,4-dioxane (2 ml). The mixture was degassed by N2 for 5 mm, then heated at 100C for 24 h. Concentrate to remove solvents. The afforded crude was purified with normal phase silica gel chromatography (0 to 100% EtOAc in 1:1 mixed hexanes/DCM) to give desired product (as a mixture of 2).

The synthetic route of 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME CORP.; CHELLIAH, Mariappan; CHU, Hong Dong; COX, Jason, M.; DEBENHAM, John, S; EAGEN, Keith; LAN, Ping; LONDON, Clare; PLOTKIN, Michael, A.; SHAH, Unmesh; SINZ, Christopher Joseph; SUN, Zhongxiang; VACCARO, Henry, M.; VENKATRAMAN, Skikanth; WO2014/59232; (2014); A2;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Reference of 468075-00-5,Some common heterocyclic compound, 468075-00-5, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, molecular formula is C7H3BrClF3O, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

(a) 2-Chloro-5-trifluoromethoxy-benzoic acid methyl ester A mixture of 2-bromo-1-chloro-4-trifluoromethoxy-benzene (5 g, 18.2 mmol), triethylamine (5.51 g, 54.5 mmol), and Pd(dppf)Cl2 (1.33 g, 1.82 mmol) in methanol (200 mL) was stirred at 80 C. under carbon monoxide (50 Psi) overnight, filtered, and concentrated under vacuum. The residue was purified by silica gel chromatography (5% EtOAc in petroleum ether) to give the title intermediate as a colorless liquid (3.4 g, 74% yield).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, its application will become more common.

Reference:
Patent; LONG, Daniel D.; MCKINNELL, Robert Murray; JIANG, Lan; LOO, Mandy; LEPACK, Kassandra; VAN ORDEN, Lori Jean; OGAWA, Gavin; HUANG, Xiaojun; ZHANG, Weijiang; US2013/115194; (2013); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 468075-00-5, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, This compound has unique chemical properties. The synthetic route is as follows., Formula: C7H3BrClF3O

General procedure: To a solution of Compound 6A (138 mg, 0.32 mmol) in tolunen (4 mL) was added N-methylpiperazine (160 mg, 1.6 mmol), t-BuONa (61 mg, 0.64 mmol), Pd2(dba)3 (29 mg, 0.032 mmol), and Xantphos (37 mg, 0.064 mmol) and heated in a microwave oven at 120 C for 2 hours. The mixture was concentrated and purified by reverse phase column chromatography to afford Compound 6B. LC-MS (ESI) m/z: 440 [M+H]+.

According to the analysis of related databases, 468075-00-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; BIOMARIN PHARMACEUTICAL INC.; WANG, Bing; CHAO, Qi; (737 pag.)WO2019/133770; (2019); A2;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Reference of 468075-00-5, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 468075-00-5 as follows.

A mixture of 2-bromo-1-chloro-4-(trifluoromethoxy)benzene (5.00 g, 18.15 mmol), Pd(dppf)Cl2.CH2Cl2 (1.48 g, 1.82 mmol) and Et3N (7.55 mL, 54.45 mmol) in EtOH (30.00 mL) was degassed, and refilled with CO. The reaction was stirred under CO (50 psi) for 16 hours at 80 C. The reaction mixture was diluted with EtOH (20 mL), filtered through Celite, concentrated, and purified by flash chromatography on silica gel (EtOAc in PE = 0% ~ 5%) to afford A-94 (2.40 g, 8.93 mmol) as an oil. H NMR (400MHz, CDC13) _ = 7.66 – 7.59 (m, 1H), 7.42 (d, 1H), 7.24 – 7.19 (m, 1H), 4.36 (q, 2H), 1.35 (t, 3H).

According to the analysis of related databases, 468075-00-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; PRAXIS PRECISION MEDICINES, INC.; REDDY, Kiran; MARTINEZ BOTELLA, Gabriel; GRIFFIN, Andrew, Mark; MARRON, Brian, Edward; (364 pag.)WO2018/98499; (2018); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 468075-00-5, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene belongs to chlorides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 468075-00-5

mixture of 2-bromo-l-chloro-4-(trifluoromethoxy)benzene (5.00 g, 18.15 mmol), Pd(dppf)Cl2.CH2Cl2 (1.48 g, 1.82 mmol) and Et3N (5.51 g, 54.45 mmol) in EtOH (30 mL) was degassed, and refilled with CO. The reaction was stirred under CO (50 psi) for 16 hours at 80 C, at which point the desired product was observed by LCMS. The reaction mixture was diluted with EtOH (20 mL), and filtered through a Celite pad. The filtrate was concentrated. The residue was purified by flash chromatography on silica gel (EtOAc in PE = 0% ~ 5%) to afford compound 12-b (2.40 g, 8.93 mmol) as an oil. 1H NMR (400MHz, CDC13) deltaEta = 7.66 – 7.59 (m, 1H), 7.42 (d, 1H), 7.24 – 7.19 (m, 1H), 4.36 (q, 2H), 1.35 (t, 3H).

The synthetic route of 468075-00-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; PRAXIS PRECISION MEDICINES, INC.; REDDY, Kiran; MARTINEZ BOTELLA, Gabriel; GRIFFIN, Andrew, Mark; MARRON, Brian, Edward; (141 pag.)WO2018/98491; (2018); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics