Category: 111771-08-5

Adding a certain compound to certain chemical reactions, such as: 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, belongs to iodides-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 111771-08-5, Recommanded Product: 111771-08-5

To a 200 ml_ round- bottomed flask were added 2-fluoro-6-iodo-benzoic acid (7.5 g, 28.2 mmol), LiOH»H2O (1 .42 g, 33.8 mmol), and THF (100 ml_). The resulting mixture was warmed to 50 C and stirred for 2 h. Dimethyl sulfate (4.03 ml_, 42.3 mmol) was then added and the mixture was warmed to 65 C. After 2 h, the mixture was cooled to room temperature and NH4CI(aq) (50 ml_, 13 wt% solution) was added. The two resulting layers were thoroughly mixed and then separated. The organic layer was dried over MgSO4, filtered, and concentrated under reduced pressure to a light brown oil (7.79 g, 99% yield). 1H NMR (400 MHz, CDCIs): 7.68 – 7.60 (m, 1 H), 7.15 – 7.06 (m, 2H), 3.98 (s, 3H).

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, 2-Fluoro-6-iodobenzoic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; BRANSTETTER, Bryan, James; LETAVIC, Michael, A.; LY, Kiev, S.; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.; WO2011/50200; (2011); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Synthetic Route of 111771-08-5, The chemical industry reduces the impact on the environment during synthesis 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, I believe this compound will play a more active role in future production and life.

Step A: 2-Fluoro-6-iodo-benzoic acid methyl ester. To a 200 mL round- bottomed flask were added 2-fluoro-6-iodo-benzoic acid (7.5 g, 28.2 mmol), LiOH*H2O (1 .42 g, 33.8 mmol), and THF (100 mL). The resulting mixture was warmed to 50 C and stirred for 2 h. Dimethyl sulfate (4.03 mL, 42.3 mmol) was then added and the mixture was warmed to 65 C. After 2 h, the mixture was cooled to room temperature and NH4CI(aq) (50 mL, 13 wt% solution) was added. The two resulting layers were thoroughly mixed and then separated. The organic layer was dried over MgSO4, filtered, and concentrated under reduced pressure to a light brown oil (7.79 g, 99% yield). 1H NMR (400 MHz, CDCIs): 7.68 – 7.60 (m, 1 H), 7.15 – 7.06 (m, 2H), 3.98 (s, 3H).

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, 2-Fluoro-6-iodobenzoic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; BRANSTETTER, Bryan, James; LETAVIC, Michael, A.; LY, Kiev, S.; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.; WO2011/50202; (2011); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Some common heterocyclic compound, 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, molecular formula is C7H4FIO2, 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. Recommanded Product: 111771-08-5

To a round-bottomed flask equipped with an overhead magnetic stirrer, reflux condenser, and nitrogen inlet were added 2-Fluoro-6-iodobenzoic acid (2.5 g, 9.4 mmol), Cul (0.09 g, 0.47 mmol), and CS2CO3 (6.1 g, 18.8 mmol). To these solids were added dioxane (12.5 ml_), water (0.05 ml_), 1 H-1 ,2,3-triazole (1.09 ml_, 18.8 mmol), and finally (1 R,2R)-N1 ,N2-dimethylcyclohexane-1 ,2-diamine (0.3 ml_, 1.88 mmol). The mixture was then warmed to 100 C ON. The day after the mixture was cooled and MTBE and water were added. After vigorous mixing, the layers were separated and the bottom aqueous layer was acidified to pH 2 with 6N HCI. The aqueous phase was then extracted with DCM (3x). The combined organic layers were dried, and concentrated The residue was purified by FC on S1O2 column (eluent : from DCM to DCM:MeOH 90:10) to afford 2-fluoro-6-(2H-1 ,2,3-triazol-2-yl)benzoic acid (p186, 1.1 g, y= 56%). MS (m/z): 208.0 [M+H]+

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 111771-08-5, its application will become more common.

Reference:
Patent; CHRONOS THERAPEUTICS LIMITED; MICHELI, Fabrizio; BERTANI, Barbara; GIBSON, Karl Richard; DI FABIO, Romano; RAVEGLIA, Luca; ZANALETTI, Riccardo; CREMONESI, Susanna; POZZAN, Alfonso; SEMERARO, Teresa; TARSI, Luca; LUKER, Timothy Jon; (275 pag.)WO2019/43407; (2019); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Electric Literature of 111771-08-5,Some common heterocyclic compound, 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, molecular formula is C7H4FIO2, 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 200 mL round- bottomed flask were added 2-fluoro-6-iodo-benzoic acid (7.5 g, 28.2 mmol), LiOH*H2O (1 .42 g, 33.8 mmol), and THF (100 mL). The resulting mixture was warmed to 50 oC and stirred for 2 h. Dimethyl sulfate (4.03 mL, 42.3 mmol) was then added and the mixture was warmed to 65 oC. After 2 h, the mixture was cooled to room temperature and NH CI(ac?) (50 mL, 13 wt% solution) was added. The two resulting layers were thoroughly mixed and then separated. The organic layer was dried over MgSO4, filtered, and concentrated under reduced pressure to a light brown oil (7.79 g, 99% yield). 1H NMR (400 MHz, CDCIs): 7.68 – 7.60 (m, 1 H), 7.15 – 7.06 (m, 2H), 3.98 (s, 3H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Fluoro-6-iodobenzoic acid, its application will become more common.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; CHAI, Wenying; LETAVIC, Michael, A.; LY, Kiev, S.; PIPPEL, Daniel, J.; RUDOLPH, Dale, A.; SAPPEY, Kathleen, C.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.; SOYODE-JOHNSON, Akinola; STOCKING, Emily, M.; SWANSON, Devin, M.; WO2011/50198; (2011); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Electric Literature of 111771-08-5, These common heterocyclic compound, 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, 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.

EXAMPLE 2-78 4-Chloro-5-fluoro-3-methyl-1-(2-pyridinyl)-1H-pyrazolo[3,4-b]quinoline Following the procedures described in Reference Example 2-5 and Example 2-1, the title compound was prepared from 2-fluoro-6-iodobenzoic acid and 3-methyl-1-(2-pyridinyl)-1H-pyrazol-5-ylamine (51% yield). mp: 160-161 C. (recrystallized from ethyl acetate). NMR (CDCl3) delta: 3.01 (3H, s), 7.14-7.29 (2H, m), 7.63-7.76 (1H, m), 7.88-8.01 (2H, m), 8.65-8.78 (2H, m).

Statistics shows that 2-Fluoro-6-iodobenzoic acid is playing an increasingly important role. we look forward to future research findings about 111771-08-5.

Reference:
Patent; Uchikawa, Osamu; Mitsui, Keita; Asakawa, Akiko; Morimoto, Shigeru; Yamamoto, Masataka; Kimura, Hiroyuki; Moriya, Takeo; Mizuno, Masahiro; US2003/187014; (2003); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, A new synthetic method of this compound is introduced below., Recommanded Product: 111771-08-5

A suspension of 2-fluoro-6-iodobenzoic acid (300 mg, 1 .1 mmol), (1 R,2R)-N,N- dimethylcyclohexane-1 ,2-diamine (32 mg, 0.23 mmol), Cs2C03 (735 mg, 2.3 mmol), 1 H- 1 ,2,3-triazole (0.13 mL, 2.3 mmol), water (0.01 mL) in 1 ,4-dioxane (5 mL) was degassed under nitrogen for 10 mins. Cul (10.7 mg, 0.06 mmol) was added and the mixture was further degassed under nitrogen for 10 mins. The pressure tube was sealed and the mixture was heated to 100 for 18 hrs. After cooling, the reaction mixture was quenched with 13%wt NaCI in 2.5M hydrochloric acid (50 mL) and extracted with EtOAc. The combined organics were dried over MgSO4, filtered and concentrated in vacuo. The crude product was purified by chromatography on the Biotage Isolera Four (25 g column, 0 to 75% (10% AcOH in EtOAc) in heptane) to afford the title compound as an oil (140 mg). 1H NMR (250 MHz, MeOD) 7.94 (s, 2 H), 7.80 (m, 1 H), 7.62 (m, 1 H), 7.29 (m, 1 H).

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; C4X DISCOVERY LIMITED; BLANEY, Emma Louise; MARTIN, Barrie Phillip; NOWAK, Thorsten; WATSON, Martin John; (212 pag.)WO2016/34882; (2016); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, belongs to iodides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. COA of Formula: C7H4FIO2

EXAMPLE 2-162 4-Chloro-5-fluoro-1-(2-pyridinyl)-1H-pyrazolo[3,4-b]quinoline Following the procedures described in Reference Example 2-5 and Example 2-1, the title compound was prepared from 2-fluoro-6-iodobenzoic acid and 1-(2-pyridinyl)-1H-pyrazol-5-ylamine (64% yield). mp: 173-176 C. (recrystallized from ethyl acetate). NMR (CDCl3) delta: 7.18-7.34 (2H, m), 7.66-7.79 (1H, m), 7.92-8.07 (2H, m), 8.62 (1H, s), 8.66-8.73 (2H, m).

The synthetic route of 111771-08-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Uchikawa, Osamu; Mitsui, Keita; Asakawa, Akiko; Morimoto, Shigeru; Yamamoto, Masataka; Kimura, Hiroyuki; Moriya, Takeo; Mizuno, Masahiro; US2003/187014; (2003); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, belongs to iodides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. COA of Formula: C7H4FIO2

To a heterogeneous mixture of 2-fluoro-6-iodobenzoic acid (1 .51 g, 5.66 mmol) at 0 C in DCM (28 mL) was added oxalyl chloride (0.635 mL, 7.36 mmol) followed by DMF (0.15 mL). Gas evolution commenced immediately and after 5 min the ice bath was removed. When gas evolution had ceased and the mixture was homogeneous an aliquot was removed and quenched with MeOH. Formation of the methyl ester was confirmed by HPLC and the mixture was concentrated in vacuo. The viscous liquid was dissolved in fresh DCM (28 mL) and treated with solid N-hydroxyacetamidine (503 mg, 6.79 mmol) in several portions followed by TEA (1 .2 mL, 8.49 mmol) at 0 C. After stirring for 14 h at ambient temperature the mixture was washed with saturated aqueous NaHCO3 solution. The combined organic extracts were dried over Na2SO4, filtered andconcentrated in vacuo. Chromatography (Hex to 100% EtOAc/Hex) afforded the desired product as a colorless oil (1 .57 g, 86%). MS (ESI) mass calculated for C9H8FIN2O2, 321 .96; m/z found, 323.0. 1 H NMR (500 MHz, CDCI3): 7.70 – 7.65 (m, 1 H), 7.15 – 7.1 1 (m, 2H), 4.87 (br s, 2H), 2.06 (s, 3H).

The synthetic route of 111771-08-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; BRANSTETTER, Bryan, James; LETAVIC, Michael, A.; LY, Kiev, S.; RUDOLPH, Dale, A.; SAVALL, Brad, M.; SHAH, Chandravadan, R.; SHIREMAN, Brock, T.; WO2011/50200; (2011); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Some common heterocyclic compound, 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, molecular formula is C7H4FIO2, 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. Formula: C7H4FIO2

(2-Fluoro-6-iodophenyl)methanol.; To a stirred solution of 2-fluoro-6-iodobenzoic acid (10 mmol) in THF (6.5 mL) and trimethylborate (3.25 mL) was added borane dimethylsulfide (12 mmol) slowly, maintaining the internal temperature at 20-25 C. Stirring was continued for an additional 16 h at room temperature and then methanol (1.44 mL) was added cautiously. The resulted solution was evaporated in vacuo to offer 2.5 g of the title compound as a pale yellow oil.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 111771-08-5, its application will become more common.

Reference:
Patent; PHARMACOPEIA, INC.; US2008/85898; (2008); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Adding a certain compound to certain chemical reactions, such as: 111771-08-5, name is 2-Fluoro-6-iodobenzoic acid, belongs to iodides-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 111771-08-5, Quality Control of 2-Fluoro-6-iodobenzoic acid

Intermediate 21: 2-Fluoro-6-(2H-l,2,3-triazol-2-yl)benzoic acid To a solution of 2H-l,2,3-triazole (5.0 g, 72.46 mmol ) in DMF (20 ml) was added cesium carbonate (23.55 g, 72.46 mmol), N,N-dimethylethylenediamine (1.02 g, 7.24 mmol), copper(I) iodide (0.34 g, 1.811 mmol) and 2-fluoro-6-iodobenzoic acid (9.63 g, 36.23 mmol ) at 0-10 C. The reaction was stirred at 125C for 15 min in the microwave and then poured into water (100 ml) and extracted with ethyl acetate (100 ml x 3). The aqueous layer was acidified with dilute HC1 to pH 2 and extracted with ethyl acetate (100 ml x 3). The combined organic layer was washed with brine, dried over sodium sulphate and concentrated in vacuo. This was then purified by column chromatography (0-3% methanol / dichloromethane) to afford the title compound.1H NMR (400 MHz DMSO- d6): delta ppm 7.43-7.47 (m, 1H), 7.66-7.72 (m, 1H), 7.78-7.80 (m, 1H), 8.13 (s, 2H), 13.71 (s, 1H)MS ES+: 208

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it.

Reference:
Patent; TAKEDA CAMBRIDGE LIMITED; TAKEDA PHARMACEUTICAL COMPANY LIMITED; FIELDHOUSE, Charlotte; GLEN, Angela; ROBINSON, John Stephen; FUJIMOTO, Tatsuhiko; WO2015/55994; (2015); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com