Category: 115843-99-7

Application of 115843-99-7, The chemical industry reduces the impact on the environment during synthesis 115843-99-7, name is 4-Bromo-3-chloro-2-fluoroaniline, I believe this compound will play a more active role in future production and life.

Anhydrous DMF (60 ml_) is added to a flask charged with bromide 9a (5.00 g, 22.2 mmol), Jb/s-(pinacolato)diborane (8.48 g, 33.4 mmol) and potassium acetate (6.35 g, 66.8 mmol) and the resulting suspension is deoxygenated by bubbling a stream of N2 gas through the mixture for 45 min. 1 ,1′-bis(diphenylphosphino)ferrocene (2.73 g, 3.34 mmol) is then added and the mixture is deoxygenated for approximately a further 5 min and is then heated to 950C. After 16 h, the dark reaction mixture is cooled, extracted with EtOAc (500 ml. and 300 ml.) and washed with 1:1 water/brine (600 mL) and brine (600 ml_). The combined extracts are dried over anhydrous MgSO4, filtered and evaporated to a black syrup which is purified by flash column chromatography (EtOAc / hexane) to afford the boronate 9b as white solid contaminated with <25 % of the diboron reagent (4.24 g, 62% yield). In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 4-Bromo-3-chloro-2-fluoroaniline, other downstream synthetic routes, hurry up and to see. Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GmbH; WO2009/62289; (2009); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthetic Route of 115843-99-7, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 115843-99-7 name is 4-Bromo-3-chloro-2-fluoroaniline, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

Anhydrous DMF (60 ml.) is added to a flask charged with bromide 9a (5.00 g, 22.2 mmol), jb/s-(pinacolato)diboron (8.48 g, 33.4 mmol) and potassium acetate (6.35 g, 66.8 mmol) and the resulting suspension is deoxygenated by bubbling a stream of N2 gas through the mixture for about 45 min. 1 , 1 ‘-bis(diphenylphosphino)ferrocene (2.73 g, 3.34 mmol) is then added and the mixture is deoxygenated for approximately a further 5 min and is then heated to 950C. After about 16 h, the dark reaction mixture is cooled, extracted with EtOAc (500 mL and 300 mL) and washed with 1 :1 water/brine (600 ml.) and brine (600 mL). The combined extracts are dried over anhydrous MgSO4, filtered and evaporated to a black syrup which is purified by flash column chromatography (EtOAc / hexanes) to afford the boronate 9b as white solid contaminated with <25 % of the diboron reagent (4.24 g, 62% yield). At the same time, in my other blogs, there are other synthetic methods of this type of compound, 4-Bromo-3-chloro-2-fluoroaniline, and friends who are interested can also refer to it. Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GmbH; WO2009/62308; (2009); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Some common heterocyclic compound, 115843-99-7, name is 4-Bromo-3-chloro-2-fluoroaniline, molecular formula is C6H4BrClFN, 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 4-Bromo-3-chloro-2-fluoroaniline

To a solution of 4-bromo-3-chloro-2-fluoroaniline (25 g, 111 mmol) and di-iso-propylethylamine (48.5 ml, 278 mmol) in DCM (250 mL) cooled in an ice bath was added acetic anhydride (11 .05 ml, 117 mmol)over 1.5 h. The reaction was warmed to RT and stirred for 24 h. The reaction was washed with HCI (1 M, 250 mL), NaHCO3 (150 mL) and water (100 mL). The organic phase was dried (MgSO4) and concentrated under reduced pressure. The residue was purified by column chromatography on silica gel (gradient elution, 0-40% EtOAc/petrol) to give the title compound (23.8 g). 1H NMR (500 MHz, DMSO-de) 9.97 (5, 1H), 7.95-7.77 (m, 1H), 7.56 (dd, 1H), 2.10 (5, 3H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 115843-99-7, its application will become more common.

Reference:
Patent; OTSUKA PHARMACEUTICAL CO., LTD.; TAIHO PHARMACEUTICAL CO., LTD.; JOHNSON, Christopher Norbert; BUCK, Ildiko Maria; CHESSARI, Gianni; DAY, James Edward Harvey; FUJIWARA, Hideto; HAMLETT, Christopher Charles Frederick; HISCOCK, Steven Douglas; HOLVEY, Rhian Sara; HOWARD, Steven; LIEBESCHUETZ, John Walter; PALMER, Nicholas John; ST DENIS, Jeffrey David; TWIGG, David Geoffrey; WOODHEAD, Andrew James; (377 pag.)WO2019/167000; (2019); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Reference of 115843-99-7, These common heterocyclic compound, 115843-99-7, name is 4-Bromo-3-chloro-2-fluoroaniline, 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.

To a solution of 4-bromo-3-chloro-2-fluoro-aniline (3 g, 13.4 mmol) and HATU (10.2 g, 26.7 mmol) in DMA (30 mL) was added TEA (5.58 mL, 40.1 mmol) and 3-tert-butoxy-3-oxopropanoic acid (3.09 mL, 20.0 mmol) at RT. The mixture was stirred at 50 C for 1 h, diluted with water, and extracted with EtOAc. The organic layer was washed with brine, dried over anhydrous Na 2SO 4, filtered, and concentrated in vacuo. The residue was purified by column chromatography on silica gel (gradient elution, 30 – 70% EtOAc/hexane) to give tert-butyl 3-(4-bromo-3-chloro-2-fluoro-anilino)-3-oxo-propanoate (3.35 g).

Statistics shows that 4-Bromo-3-chloro-2-fluoroaniline is playing an increasingly important role. we look forward to future research findings about 115843-99-7.

Reference:
Patent; TAIHO PHARMACEUTICAL CO., LTD.; OTSUKA PHARMACEUTICAL CO., LTD.; SHIMAMURA, Tadashi; KATO, Ryo; MIURA, Risako; MITA, Takashi; OGAWA, Takahiro; SAGARA, Yufu; JOHNSON, Christopher Norbert; HOWARD, Steven; DAY, James Edward Harvey; ST. DENIS, Jeffrey David; LIEBESCHUETZ, John Walter; (345 pag.)WO2020/22323; (2020); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Electric Literature of 115843-99-7,Some common heterocyclic compound, 115843-99-7, name is 4-Bromo-3-chloro-2-fluoroaniline, molecular formula is C6H4BrClFN, 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.

Example 9: Synthesis of boronate fragment 9b (used in Example 43)Anhydrous DMF (60 mL) is added to a flask charged with bromide 9a (5.00 g, 22.2 mmol), /?/s-(pinacolato)diborone (8.48 g, 33.4 mmol) and potassium acetate (6.35 g, 66.8 mmol) and the resulting suspension is deoxygenated by bubbling a stream of N2 gas through the mixture for 45 min. 1 ,1′-bis(diphenylphosphino)ferrocene (2.73 g, 3.34 mmol) is then added and the mixture is deoxygenated for approximately a further 5 min and is then heated to 950C. After 16 h, the dark reaction mixture is cooled, extracted with EtOAc (500 mL and 300 mL) and washed with 1 :1 water/brine (600 mL) and brine (600 mL). The combined extracts are dried over anhydrous MgSO4, filtered and evaporated to a black syrup which is purified by flash column chromatography (EtOAc/hexanes) to afford the boronate 9b as white solid contaminated with <25 % of the diboron reagent (4.24 g, 62% yield). These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Bromo-3-chloro-2-fluoroaniline, its application will become more common. Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GmbH; WO2009/62285; (2009); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthetic Route of 115843-99-7, The chemical industry reduces the impact on the environment during synthesis 115843-99-7, name is 4-Bromo-3-chloro-2-fluoroaniline, I believe this compound will play a more active role in future production and life.

Anhydrous DMF (60 ml_) is added to a flask charged with bromide 9a (5.00 g, 22.2 mmol), Jb/s-(pinacolato)diborane (8.48 g, 33.4 mmol) and potassium acetate (6.35 g, 66.8 mmol) and the resulting suspension is deoxygenated by bubbling a stream of N2 gas through the mixture for 45 min. 1 ,1′-bis(diphenylphosphino)ferrocene (2.73 g, 3.34 mmol) is then added and the mixture is deoxygenated for approximately a further 5 min and is then heated to 950C. After 16 h, the dark reaction mixture is cooled, extracted with EtOAc (500 ml. and 300 ml.) and washed with 1:1 water/brine (600 mL) and brine (600 ml_). The combined extracts are dried over anhydrous MgSO4, filtered and evaporated to a black syrup which is purified by flash column chromatography (EtOAc / hexane) to afford the boronate 9b as white solid contaminated with <25 % of the diboron reagent (4.24 g, 62% yield). In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 4-Bromo-3-chloro-2-fluoroaniline, other downstream synthetic routes, hurry up and to see. Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GmbH; WO2009/62289; (2009); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics