Category: 628691-93-0

Related Products of 628691-93-0 ,Some common heterocyclic compound, 628691-93-0, molecular formula is C6H3ClFNO2, 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.

3.72. Compound 73: (lR,2R)-N-(6-((2-Cyano-5-ethyl-3-fluoropyridin-4-yl)(methyl)amino)-l-methyl- lH-imidazo[4,5-c]pyridin-4-yl)-2-fluorocyclopropanecarboxamide 3.72.1. Step i: Carbamic acid, N-(2-chloro-3-fluoro-4-pyridinyl)-l,l-dimethylethyl ester To a mixture of 2-chloro-3-fluoronicotinic acid (3.55 g, 20.2 mmol, 1.0 eq), TEA (8.4 mL, 60.6 mmol, 3.0 eq) in a mixture of dry toluene (40 mL) and dry T^uOH (40 mL) under nitrogen, is added diphenylphosphoryl azide (DPPA) (6.51 mL, 30.1 mmol, 1.5 eq). The reaction is heated to 110C for 2 h. The reaction is diluted with water and the compound is extracted with DCM. The organic layer is dried over Na2S04, filtered and removed the solvent under vacuum. The residue is purified by silica chromatography (ethyl acetate/DCM, from 0-20% in 15CV) to give the desired product as transparent oil.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,628691-93-0, its application will become more common.

Reference:
Patent; GALAPAGOS NV; MENET, Christel, Jeanne, Marie; MAMMOLITI, Oscar; QUINTON, Evelyne; JOANNESSE, Caroline, Martine, Andree-Marie; DE BLIECK, Ann; BLANC, Javier; (263 pag.)WO2017/12647; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 628691-93-0 ,Some common heterocyclic compound, 628691-93-0, molecular formula is C6H3ClFNO2, 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.

3.72. Compound 73: (lR,2R)-N-(6-((2-Cyano-5-ethyl-3-fluoropyridin-4-yl)(methyl)amino)-l-methyl- lH-imidazo[4,5-c]pyridin-4-yl)-2-fluorocyclopropanecarboxamide 3.72.1. Step i: Carbamic acid, N-(2-chloro-3-fluoro-4-pyridinyl)-l,l-dimethylethyl ester To a mixture of 2-chloro-3-fluoronicotinic acid (3.55 g, 20.2 mmol, 1.0 eq), TEA (8.4 mL, 60.6 mmol, 3.0 eq) in a mixture of dry toluene (40 mL) and dry T^uOH (40 mL) under nitrogen, is added diphenylphosphoryl azide (DPPA) (6.51 mL, 30.1 mmol, 1.5 eq). The reaction is heated to 110C for 2 h. The reaction is diluted with water and the compound is extracted with DCM. The organic layer is dried over Na2S04, filtered and removed the solvent under vacuum. The residue is purified by silica chromatography (ethyl acetate/DCM, from 0-20% in 15CV) to give the desired product as transparent oil.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,628691-93-0, its application will become more common.

Reference:
Patent; GALAPAGOS NV; MENET, Christel, Jeanne, Marie; MAMMOLITI, Oscar; QUINTON, Evelyne; JOANNESSE, Caroline, Martine, Andree-Marie; DE BLIECK, Ann; BLANC, Javier; (263 pag.)WO2017/12647; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of 628691-93-0, 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. 628691-93-0, name is 2-Chloro-3-fluoroisonicotinic acid. A new synthetic method of this compound is introduced below.

Step 1: To a solution of 2-chloro-3-fluoroisonicotinic acid (5.0 g, 28 mmol) and 4-methyl morpholine (3.8 mL, 7.0 mmol) in dry THF (150 mL) was added isobutyl chloroformate (4.5 mL, 34 mmol) dropwise at 0 C and stirred for 1 h. The reaction mixture was diluted with THF (50 mL) and filtered through Celite. The filtrate was cooled to 0 C, NaBH4 (1.0 g, 28 mmol) was added, and the resulting mixture was stirred for 30 min. The reaction mixture was quenched with 10 % KHSO4 (5 mL). The volatiles were removed under reduced pressure and the reaction mixture was diluted with EtOAc (200 mL). The layers were separated and the organic layer was washed with water (50 mL) followed by sat. NaHCCb (2 x 50 mL), dried over MgSC>4, filtered and concentrated under reduced pressure. The residue was triturated with 5: 1 hexane-ether (50 mL). The resulting solid was filtered and collected to give (2- chloro-3-fluoropyridin-4-yl)methanol (3.7 g, 80%). MS (ES+) C6H5C1FNO requires: 161, found: 162 [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,628691-93-0, its application will become more common.

Reference:
Patent; TESARO, INC.; JONES, Philip; CZAKO, Barbara; BURKE, Jason P.; CROSS, Jason; LEONARD, Paul Graham; TREMBLAY, Martin; MANDAL, Pijus; (232 pag.)WO2018/119387; (2018); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 628691-93-0, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 628691-93-0, name is 2-Chloro-3-fluoroisonicotinic acid. This compound has unique chemical properties. The synthetic route is as follows.

Diphenylphosphoryl azide (DPPA) (129 mmol) wasadded to a mixture of 2-chloro-3-fluoro-pyridine-4-carbox- ylic acid (85.7 mmol), Et3N (257 mmol) in 1:1 tert-l3uOH/ toluene (200 mE). The mixture was heated at 110 C. for 4 h. Mixture was diluted with H20 and extracted with DCM. The organic layer was dried (Na2504) and concentrated. The residue was purified by flash column chromatography (5i02, 100:0 to 80:20 DCM/EtOAc) to yield the desired product tert-butyl N-(2-chloro-3-fluoro-4-pyridyl)carbamate.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 628691-93-0, 2-Chloro-3-fluoroisonicotinic acid.

Reference:
Patent; GALAPAGOS NV; Menet, Christel Jeanne Marie; Mammoliti, Oscar; Blanc, Javier; Orsulic, Mislav; Roscic, Maja; (81 pag.)US9440929; (2016); B2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 628691-93-0, 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 628691-93-0 as follows.

2-Chloro-N-(4-(4,4-difluoropiperidin-1-yl)pyridin-3-yl)-3-fluoroisonicotinamideIn a 15 mL vial was dissolved 4-(4,4-difiuoiOpiperidin-l- yl)pyridin-3-amine (139 mg, 0.650 mmol) and 2-chloro-3-fluoroisonicotinic acid (103.8 mg, 0.591 mmol) in dimethylformamide (4 mL) to give a tan solution. HATU (450 mg, 1.183 mmol) and Hunig’s base (0,207 mL, 1,183 mmol) were added, and the mixture was stirred at rt for 22 h. It was diluted with water and extracted with ethyl acetate. The organic layer was washed with brine, dried and concentrated. The residue was purified using silica gel flash chromatography, eluting with 50% ethyl acetate/hexane to afford the desired product (31.8 mg, 14.5%) as a tan oil: MS (ESI) (m/z) 371 (M+H)+; 1H NM (400 MHz, MeOD) delta 9.14 (s, lH)t 8.37 (d, J = 5.0 Hz, 1H), 8.30 (dd, J = 4.6, 3.7 Hz, 1H), 7.81 (t, J = 4.9 Hz, 1H), 7.39 (dd, J = 8.4, 4.4 Hz, 1H), 7.19 (d, J = 5.8 Hz, 1H), 3.38 – 3.31 (m, 2H), 3.25 – 3.18 (m, 2H), 2.16 – 2.02 (m, 2H), 2.01 – 1.91 (m, 2H); 1 F NMR (376 MHz, MeOD) delta -73.28 (s), -75.17 (s).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,628691-93-0, its application will become more common.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; LUO, Guanglin; CHEN, Ling; DUBOWCHIK, Gene M.; JACUTIN-PORTE, Swanee E.; SIVAPRAKASAM, Prasanna; MACOR, John E.; WO2015/69593; (2015); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 628691-93-0, name is 2-Chloro-3-fluoroisonicotinic acid, the common compound, a new synthetic route is introduced below. Computed Properties of C6H3ClFNO2

Example 125: 3-(4-Bromo-2-fluoro-phenylamino)-2-chloro-isonicotinic acid; 2-Chloro-3-fluoro-isonicotinic acid (200mg, 1.14mmol) and 4-bromo-2-fluoroaniline (217mg, 1.14mmol) were added to 5ml of dry THF and the mixture was cooled to -78 0C. LiHMDS (1 M in THF, 4.0ml) was added and the mixture was allowed to warm to room temperature over night. Solid ammonium hydrochloride (1g) was added and after 1h the mixture was filtered and the volatiles were removed in vacuo. The crude material was purified by flash-chromatography using a gradient of 0-12% methanol (containig 0.5% EPO formic acid) in DCM as eluent to give 213mg (0.617mmol; 54% yield) of pure desired carboxylic acid product. LC-MS (method IiI): rt = 4.42min; m/z [M+H]+ 386/388.

The synthetic route of 628691-93-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.; WO2006/45514; (2006); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 628691-93-0, name is 2-Chloro-3-fluoroisonicotinic acid, the common compound, a new synthetic route is introduced below. Computed Properties of C6H3ClFNO2

Example 125: 3-(4-Bromo-2-fluoro-phenylamino)-2-chloro-isonicotinic acid; 2-Chloro-3-fluoro-isonicotinic acid (200mg, 1.14mmol) and 4-bromo-2-fluoroaniline (217mg, 1.14mmol) were added to 5ml of dry THF and the mixture was cooled to -78 0C. LiHMDS (1 M in THF, 4.0ml) was added and the mixture was allowed to warm to room temperature over night. Solid ammonium hydrochloride (1g) was added and after 1h the mixture was filtered and the volatiles were removed in vacuo. The crude material was purified by flash-chromatography using a gradient of 0-12% methanol (containig 0.5% EPO formic acid) in DCM as eluent to give 213mg (0.617mmol; 54% yield) of pure desired carboxylic acid product. LC-MS (method IiI): rt = 4.42min; m/z [M+H]+ 386/388.

The synthetic route of 628691-93-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.; WO2006/45514; (2006); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of 628691-93-0 ,Some common heterocyclic compound, 628691-93-0, molecular formula is C6H3ClFNO2, 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.

Carbonyldiimidazole (1.80 g, 1 1.1 mmol) was added to a solution of 2-chloro-3-fluoro- isonicotinic acid (1.3 g, 7.41 mmol) in THF (21.2 mL). The reaction mixture was stirred at RT overnight and was then added to a cold (0C) solution of NaBH4 (1.40 g, 37 mmol) in water (52.9 mL). The mixture was stirred for 10 min at 0C, and 1 M HCI was then added carefully to quench the reaction (caution: H2 evolving). Volatiles were removed via rotary evaporation and the residue was dissolved in saturated aqueous NaHC03. The mixture was extracted repeatedly with CH2CI2, the combined organics were dried (phase separator) and concentrated in vaccuo. Purification by flash column chromatography on silica gel (eluent gradient: c- hexane/EtOAc 4: 1 to 2: 1) afforded the title compound as a white solid. TLC, Rf (c- hexane/EtOAc 1 :1) = 0.37; MS (LC/MS): 162.0 [M+H]+; tR (HPLC conditions b): 1.60 min.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,628691-93-0, its application will become more common.

Reference:
Patent; NOVARTIS AG; ALTMANN, Eva; HOMMEL, Ulrich; LORTHIOIS, Edwige Liliane Jeanne; MAIBAUM, Juergen Klaus; OSTERMANN, Nils; QUANCARD, Jean; RANDL, Stefan Andreas; SIMIC, Oliver; VULPETTI, Anna; ROGEL, Olivier; WO2012/93101; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.628691-93-0, name is 2-Chloro-3-fluoroisonicotinic acid, molecular formula is C6H3ClFNO2, molecular weight is 175.55, as common compound, the synthetic route is as follows.Product Details of 628691-93-0

Step l :A suspension of 2-chloro-3-fluoropyridine-4-carboxylic acid (CAS 628691-93-0, 2 g, 11.39 mmol) in MeOH (7 mL) and DCM (21 mL) at 0 C was treated with TMS-Diazomethane (5.70 mL, 11.39 mmol) in a drop wise fashion. The reaction was stirred at 0 C for 0.5 h. The reaction was quenched with AcOH (0.5 mL) and concentrated in vacuo. The residue was purified by flash chromatography (0-100% EtOAc in petrol on Si02) to afford methyl 2-chloro-3-fluoropyridine-4-carboxylate. 1H NMR (300 MHz, Methanol-^) delta ppm 3.97 (s, 3 H) 7.76 – 7.86 (m, 1 H) 8.29 – 8.40 (m, 1 H)

At the same time, in my other blogs, there are other synthetic methods of this type of compound,628691-93-0, 2-Chloro-3-fluoroisonicotinic acid, and friends who are interested can also refer to it.

Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; AHMED, Saleh; BARKER, Gregory; CANNING, Hannah; DAVENPORT, Richard; HARRISON, David; JENKINS, Kerry; LIVERMORE, David; WRIGHT, Susanne; KINSELLA, Natasha; (259 pag.)WO2016/148306; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of 628691-93-0 ,Some common heterocyclic compound, 628691-93-0, molecular formula is C6H3ClFNO2, 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.

Carbonyldiimidazole (1.80 g, 1 1.1 mmol) was added to a solution of 2-chloro-3-fluoro- isonicotinic acid (1.3 g, 7.41 mmol) in THF (21.2 mL). The reaction mixture was stirred at RT overnight and was then added to a cold (0C) solution of NaBH4 (1.40 g, 37 mmol) in water (52.9 mL). The mixture was stirred for 10 min at 0C, and 1 M HCI was then added carefully to quench the reaction (caution: H2 evolving). Volatiles were removed via rotary evaporation and the residue was dissolved in saturated aqueous NaHC03. The mixture was extracted repeatedly with CH2CI2, the combined organics were dried (phase separator) and concentrated in vaccuo. Purification by flash column chromatography on silica gel (eluent gradient: c- hexane/EtOAc 4: 1 to 2: 1) afforded the title compound as a white solid. TLC, Rf (c- hexane/EtOAc 1 :1) = 0.37; MS (LC/MS): 162.0 [M+H]+; tR (HPLC conditions b): 1.60 min.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,628691-93-0, its application will become more common.

Reference:
Patent; NOVARTIS AG; ALTMANN, Eva; HOMMEL, Ulrich; LORTHIOIS, Edwige Liliane Jeanne; MAIBAUM, Juergen Klaus; OSTERMANN, Nils; QUANCARD, Jean; RANDL, Stefan Andreas; SIMIC, Oliver; VULPETTI, Anna; ROGEL, Olivier; WO2012/93101; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem