Category: 64248-58-4

Some common heterocyclic compound, 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, molecular formula is C6H3F2I, 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. name: 1,2-Difluoro-4-iodobenzene

A mixture of methyl indole-5-carboxylate Ij (2 g, 11.4 mmol), l-iodo-3,4-difluoro-benzene Io (1.5 mL, 12.5 mmol), CuI (0.22 g, 1.14 mmol), trans-N, N’-dimethylcyclohexane-l,2- diamine (0.54 mL, 3.43 mmol), and K3PO4 (6.06 g, 28.5 mmol) in toluene (12 mL) was heated at 110 0C for 7 hours. The reaction mixture was diluted with CH2CI2 and filtered. The solution was concentrated and the residue was purified by flash column chromatography (silica gel, 20% EtOAc/heptane) to give Ip (3.0 g).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 64248-58-4, its application will become more common.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; BIAN, Haiyan; CHEVALIER, Kristen, M.; CONNOLLY, Peter, J.; FLORES, Christopher, M.; LIN, Shu-chen; LIU, Li; MABUS, John; MACIELAG, Mark, J.; MCDONNELL, Mark, E.; PITIS, Philip, M.; ZHANG, Sui-po; ZHANG, Yue-mei; ZHU, Bin; CLEMENTE, Jose; WO2010/124082; (2010); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

64248-58-4, name is 1,2-Difluoro-4-iodobenzene, 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. Formula: C6H3F2I

A mixture of methyl indole-5-carboxylate 24a (2 g, 11.4 mmol), 1-iodo-3,4-difluoro-benzene 24b (1.5 mL, 12.5 mmol), CuI (0.22 g, 1.14 mmol), trans-N,N’-dimethylcyclohexane-1,2-diamine (0.54 mL, 3.43 mmol), and K3PO4 (6.06 g, 28.5 mmol) in toluene (12 mL) was heated at 110 C. for 7 hours. The reaction mixture was diluted with CH2Cl2 and filtered. The solution was concentrated and the residue was purified by flash column chromatography (silica gel, 20% EtOAc/heptane) to give 24c (3.0 g).

The synthetic route of 64248-58-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Connolly, Peter J.; Macielag, Mark J.; McDonnell, Mark E.; Zhu, Bin; US2012/77797; (2012); 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. 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, A new synthetic method of this compound is introduced below., name: 1,2-Difluoro-4-iodobenzene

In a glassware flask equipped with a condenser and a magnetic stirrer, were put 85.7 g (357 mmol) of 3,4-difluoroiodobenzene, 43.2 g (680 mmol) of copper powder, and 86 g of N-methylpyrrolidinone (NMP). The mixture was stirred under nitrogen atmosphere on an oil bath at 190 C for 5 h. After cooling to room temperature, the reaction mixture was mixed with 300 mL of tert-butyl methyl ether and filtered in order to remove copper and its salt. The filtrate was washed with water (300 mL x 3) and then with saturated aqueous sodium chloride solution (300 mL x 1), and dried with magnesium sulfate and filtered. The filtrate was evaporated and the resulting residue was column-chromatographed using hexane as an eluent to give a white solid (35 g, 87% yield) of product 4. The spectral data agreed with those of the authentic sample: 19F NMR (CDCl3) (with 1H decoupling) delta -136.88 (d, J = 21 Hz, 2F), -139.64 ppm (d, J = 21 Hz, 2F); 1H NMR (CDCl3) delta 7.25 (m, 4H), 7.34 ppm (m, 2H).

The synthetic route of 64248-58-4 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Umemoto; Zhou, Xiaocong; Li, Yuanqiang; Journal of Fluorine Chemistry; vol. 226; (2019);,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Reference of 64248-58-4,Some common heterocyclic compound, 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, molecular formula is C6H3F2I, 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.

General procedure: A Schlenk flask equipped with asepta and a magnetic stir bar wasfilled with aryl halide (3.0 mmol), alkene (3.2 mmol), K2CO3(3.5 mmol) and PdLn-beta-CD 3 mol% catalyst in water (5 mL pure orplain). The reaction was refluxed for the appropriate time underaerobic conditions. After completion of the reaction was confirmedby TLC, the reaction mixturewas cooled to room temperature.The solvent was removed by rotary evaporator and extraction of theproduct was carried out using ethyl acetate. The ethyl acetate fractionwas separated and dried over anhydrous sodium sulphate. Theresulting crude product was purified using flash column chromatographyof silica gel 60-120mesh with n-hexane/ethyl acetate (8:2ratio) as the eluent and afforded the pure desired product. After extractionof product, catalyst was simply reprecipitated from theaqueous layer by the addition of 10 mL of acetone. The recoveredcatalyst was filtered, washed with acetone (3 × 5 mL) and dried ina vacuum at 70 C for 5 h and reused.

The synthetic route of 64248-58-4 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Dindulkar, Someshwar D.; Jeong, Daham; Kim, Hwanhee; Jung, Seunho; Carbohydrate Research; vol. 430; (2016); p. 85 – 94;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Application of 64248-58-4,Some common heterocyclic compound, 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, molecular formula is C6H3F2I, 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 mixture of methyl indole-5-carboxylate 7a (2 g, 11.4 mmol), 1-iodo-3,4-difluoro-benzene 8a (1.5 mL, 12.5 mmol), CuI (0.22 g, 1.14 mmol), trans-N,N’-dimethylcyclohexane-1,2-diamine (0.54 mL, 3.43 mmol), and K3PO4 (6.06 g, 28.5 mmol) in toluene (12 mL) was heated at 110 C. for 7 h. The reaction mixture was diluted with CH2Cl2 and filtered. The solution was concentrated and the residue was purified by flash column chromatography (silica gel, 20% EtOAc/heptane) to give 3.0 g of compound 8b. MS m/z 288.1 (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 1,2-Difluoro-4-iodobenzene, its application will become more common.

Reference:
Patent; Connolly, Peter J.; Bian, Haiyan; Li, Xun; Liu, Li; Macielag, Mark J.; McDonnell, Mark E.; US2013/102584; (2013); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Some common heterocyclic compound, 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, molecular formula is C6H3F2I, 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. Computed Properties of C6H3F2I

A mixture of methyl indole-5-carboxylate Ij (2 g, 11.4 mmol), l-iodo-3,4-difluoro-benzene Io (1.5 mL, 12.5 mmol), CuI (0.22 g, 1.14 mmol), trans-N, N’-dimethylcyclohexane-l,2- diamine (0.54 mL, 3.43 mmol), and K3PO4 (6.06 g, 28.5 mmol) in toluene (12 mL) was heated at 110 0C for 7 hours. The reaction mixture was diluted with CH2CI2 and filtered. The solution was concentrated and the residue was purified by flash column chromatography (silica gel, 20% EtOAc/heptane) to give Ip (3.0 g).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 64248-58-4, its application will become more common.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; BIAN, Haiyan; CHEVALIER, Kristen, M.; CONNOLLY, Peter, J.; FLORES, Christopher, M.; LIN, Shu-chen; LIU, Li; MABUS, John; MACIELAG, Mark, J.; MCDONNELL, Mark, E.; PITIS, Philip, M.; ZHANG, Sui-po; ZHANG, Yue-mei; ZHU, Bin; CLEMENTE, Jose; WO2010/124082; (2010); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Electric Literature of 64248-58-4, 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. 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, This compound has unique chemical properties. The synthetic route is as follows.

Example 18 a) 7.40 g (62.5 mmol) of benzimidazole is added to 2.50 g (62.5 mmol) of 60 % sodium hydride in 100 ml of NMP at room temperature, then 7.50 g (31.3 mmol) of 1 ,2-difluoro-4- iodo-benzene is added at room temperature and stirred for 24 h at 190 C. The reaction mixture is cooled at room temperature and added water, then the precipitate is filterted off, washed with ethyl acetate and dried. Yield 10.8 g (79 %). 1 H NMR (400 MHz, CDCI3): delta 8.10 (d, J = 1.9 Hz, 1 H); 8.08 (dd, J = 8.3, 2.0 Hz, 1 H); 7.76 (dd, J = 7.9, 1 .1 Hz, 2H); 7.67 – 7.58 (m, 2H); 7.48 (d, J = 8.3 Hz, 1 H); 7.33 – 7.16 (m, 6H).

The chemical industry reduces the impact on the environment during synthesis 1,2-Difluoro-4-iodobenzene. I believe this compound will play a more active role in future production and life.

Reference:
Patent; IDEMITSU KOSAN CO., LTD.; SAITO, Masatoshi; NAGASHIMA, Hideaki; (118 pag.)WO2017/178864; (2017); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Reference of 64248-58-4,Some common heterocyclic compound, 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, molecular formula is C6H3F2I, 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.

Intermediate 7: Ethyl 1-(3,4-difluorophenyl)-5-methyl-1H-1 ,2,3-triazole-4-carboxylate; To a mixture of 1 ,2-difluoro-4-iodobenzene (1 g, 4.17 mmol) and ethyl 2-butynoate (0.484 ml_, 4.17 mmol) in water (0.444 ml)/DMS0 (4 ml) at room temperature were added L-proline (0.096 g, 0.833 mmol), sodium carbonate (0.088 g, 0.833 mmol), sodium azide (0.325 g, 5.00 mmol), sodium l-ascorbate (0.083 g, 0.417 mmol) and copper(ll) sulfate pentahydrate (0.052 g, 0.208 mmol) (in this order) and the mixture was heated at 65 0C overnight. On cooling to room temperature, the mixture was quenched with aqueous ammonia (1 ml) and EtOAc (20ml) and water (20 ml) were added. The two phases were separated and the aqueous phase was extracted with EtOAc (3 x 30 ml). The organic phases were combined and washed with water/brine (50ml) repeatedly. The organic phases were dried over sodium sulfate, filtered and the solvent was evaporated to afford a crude product that was purified by MDAP to afford the title compound (23.9%); MH+=267.9; 1HNMR (DMSO, 400 MHz): 1.34 (3H t), 4.36 (2H, q), 7.57 (1 H m), 7.76 (1 H m), 7.94 (1 H m).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1,2-Difluoro-4-iodobenzene, its application will become more common.

Reference:
Patent; GLAXO GROUP LIMITED; WO2009/115486; (2009); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

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. 64248-58-4, name is 1,2-Difluoro-4-iodobenzene, This compound has unique chemical properties. The synthetic route is as follows., Safety of 1,2-Difluoro-4-iodobenzene

A a solution of /Patent; CENTAURUS THERAPEUTICS; ROMERO, Donna, L.; BLITZER, Jeremy; (242 pag.)WO2019/140188; (2019); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

64248-58-4, name is 1,2-Difluoro-4-iodobenzene, 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: C6H3F2I

Add bis (triphenylphosphine) palladium (II) dichloride (110 mg, 0. 15 mmol), copper (I) iodide (57 mg, 0. 30 mmol), and 3-ethynyl-5-methoxypyridine, (prepared as described in PREPARATION 10), (400 mg, 3. 0 mmol) to a solution of 1, 2-difluoro-4- iodobenzene (0. 43 mL, 3. 6 mmol) in triethylamine (6. 3 mL, 45. 0 mmol) and heat at 60 C for 20 h. Cool to room temperature and concentrate. Purify the residue by silica gel chromatography, eluting with 100 : 0 to 65 : 35 hexanes : ethyl acetate, followed by a second silica gel chromatography, eluting with 100 : 0 to 80 : 20 dichloromethane : ethyl acetate, to give the title compound as a white solid (690 mg, 94%). 1H NMR (300 MHz, CDCl3) 6 3. 89 (s, 3H), 7. 11-7. 21 (m, 1H), 7. 28-7. 40 (m, 3H), 8. 27- 8. 30 (d, J = 2. 9 Hz, 1H), 8. 34-8. 37 (d, J = 1. 6 Hz, 1H), MS (APCI) : m/z = 246 [M+H] +.

The synthetic route of 64248-58-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ELI LILLY AND COMPANY; WO2005/94822; (2005); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com