Category: 452-79-9

Application of 452-79-9, 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. 452-79-9, name is 2-Fluoro-1-iodo-4-methylbenzene belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

Example 180 (5R)-7-(2-Fluoro-4-methylphenyl)-2-(trans-4-hydroxycyclohexyl)-2,7-diazaspiro[4.5]decan-l- one H A mixture of (5R)-2-(fralphar°-4-hydroxycyclohexyl)-2,7-diazaspiro[4.5]decan-l-one (20 mg, 0.00007 mol, this compound was prepared by using procedures analogous to those described in example 1, steps 1-5), 4-methyl-2-fluoro-l-iodobenzene (21 mg, 0.00009 mol), sodium tert-bvAoxide (9.98 mg, 0.000104 mol), 1,4,7,10,13,16-hexaoxacyclooctadecane (27.4 mg, 0.000104 mol) , 2-(di- tert-butylphosphino)biphenyl (0.8 mg, 0.000003 mol) , tris(diben2ylideneacetone)dipalladium(0) (1 mg, 0.000001 mol), in tert-butyl alcohol (1.0 mL, 0.010 mol) was stirred at rt for 18. The crude product was purified by prep-HPLC to afford the desired product. . LC-MS: 361.1 (MfH)+.

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-1-iodo-4-methylbenzene, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; INCYTE CORPORATION; WO2006/53024; (2006); A2;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Related Products of 452-79-9, 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. 452-79-9 name is 2-Fluoro-1-iodo-4-methylbenzene, 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.

N-Bromosuccinimide (2.63g, 14.78mmol) and benzoylperoxide (0.20g, 0.62mmol) were added to a solution of 3-fluoro-4-iodotoluene (2.90g, 12.29mmol) in 7mL of tetrachloromethane. The resulting solution was refluxed for 20h. Thereafter, the reaction was allowed to cool to room temperature and was then diluted with 30mL of CH2Cl2. The solid phase was filtered off and the filtrate was washed with 30mL of a saturated solution of sodium thiosulphate. The organic layer was dried over Na2SO4 and evaporated. The crude product was purified by flash chromatography (AcOEt/PE 2:98), giving 3.45g (86%) of 8 as a white solid. Rf=0.76 (AcOEt/PE 5:95); mp=46-48C. 1H NMR (600MHz, CDCl3) delta 7.71 (m, 1H), 7.11 (m, 1H), 6.94 (m, 1H), 4.41 (s, 2H); 13C NMR (150MHz, CDCl3) delta 161.0 (J=246.5Hz), 140.6 (J=7.6Hz), 139.9 (J=1.3Hz), 126.4 (J=3.2Hz), 116.4 (J=24.5Hz), 81.3 (J=25.6Hz), 31.5; 19F (564MHz, CDCl3) delta -92.9 (t, J=7.3Hz). Anal. calcd for C7H5BrFI: C, 26.70; H, 1.60; found: C, 26.70; H, 1.58.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-Fluoro-1-iodo-4-methylbenzene, and friends who are interested can also refer to it.

Reference:
Article; Castillo Melean, Johnny; Humpert, Sven; Ermert, Johannes; Coenen, Heinz H.; Journal of Fluorine Chemistry; vol. 178; (2015); p. 202 – 207;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Application of 452-79-9,Some common heterocyclic compound, 452-79-9, name is 2-Fluoro-1-iodo-4-methylbenzene, molecular formula is C7H6FI, 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 (3S)-piperidin-3-ol hydrochloride (0.50 g, 0.0036 mol), 2-fluoro-l-iodo-4- methylbenzene (1.03 g, 0.00436 mol), copper(I) iodide (140 mg, 0.00073 mol), potassium phosphate (3.08 g, 0.0145 mol), and 1,2-ethanediol (0.810 mL, 0.0145 mol) in 1-butanol (7.28 mL, 0.0796 mol) was heated at 100 0C under nitrogen for 2 nights. The reaction mixture was treated with water, and then extracted with EtOAc. The organic layers were combined, washed with brine, dried and evaporated to dryness. The residue was used directly in next step (519 mg, 69%). LCMS (M+H):210.2.

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-1-iodo-4-methylbenzene, its application will become more common.

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. 452-79-9, name is 2-Fluoro-1-iodo-4-methylbenzene belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. COA of Formula: C7H6FI

25mL reaction flask, adding 360mg (5.6mmol) copper powder, vacuuming for three times, then injecting 10mL dimethyl sulfoxide, 472mg (2mmol) 4-methyl-2-fluoroiodobenzene, 609mg (3mmol) ethyl bromodifluoroacetate, reacted at 80C overnight, the next day, the temperature was lowered to room temperature, extracted with 50 mL of ethyl acetate, washed with saturated sodium chloride solution, dried over anhydrous sodium sulfate, the solvent was distilled off by rotary evaporation to give a mixture of ethyl 2-(4-methyl 2-fluorophenyl)-2,2-difluoroacetate as a yellow liquid of 310 mg. Used directly in the next step of the reaction.

The synthetic route of 452-79-9 has been constantly updated, and we look forward to future research findings.

Related Products of 452-79-9,Some common heterocyclic compound, 452-79-9, name is 2-Fluoro-1-iodo-4-methylbenzene, molecular formula is C7H6FI, 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 3-fluoro-4-iodotoluene (2.26 g, 9.58 mmol), N-bromosuccinimide (2.03 g, 11.49 mmol) and benzoyl peroxide (5 mol %, 116 mg, 0.48 mmol) in carbon tetrachloride (5 ml) was stirred at reflux for 20 hours, cooled, diluted with dichloromethane and filtered. The purple coloured filtrate was washed with saturated sodium thiosulphate solution (aq) (20 ml). The organic layer was separated, dried over sodium sulphate and the solvent removed by rotary evaporation to give the title compound as a yellow oil (2.58 g, 86%).1H-NMR (250 MHz, CDCl3): delta 7.72 (1H, m), 7.11 (1H, m), 6.94 (1H, m), 4.41 (2H, s).

The synthetic route of 452-79-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; GLAXO GROUP LIMITED; US2010/137276; (2010); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Application of 452-79-9,Some common heterocyclic compound, 452-79-9, name is 2-Fluoro-1-iodo-4-methylbenzene, molecular formula is C7H6FI, 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: To a solution of the corresponding boronic acid (1.2mmol) in EGME/H2O (3:1, 0.25M) were added Pd(OAc)2 (0.05mmol) and K2CO3 (1.2mmol), followed by the addition of the corresponding phenyl iodide (1.0mmol). The dark reaction mixture was stirred at rt for 15h, then diluted with EtOAc (40mL) and filtered through a pad of Celite. The resulting filtrate was washed with H2O (20mL) and a 1M solution of Na2SO3 (20mL). After separation, the organic phase was dried over Na2SO4 and concentrated under reduced pressure. The residues were purified by column chromatography (Cy/EtOAc).

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-1-iodo-4-methylbenzene, its application will become more common.

Reference:
Article; Migliore, Marco; Habrant, Damien; Sasso, Oscar; Albani, Clara; Bertozzi, Sine Mandrup; Armirotti, Andrea; Piomelli, Daniele; Scarpelli, Rita; European Journal of Medicinal Chemistry; vol. 109; (2016); p. 216 – 237;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

452-79-9, 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. 452-79-9, name is 2-Fluoro-1-iodo-4-methylbenzene, A new synthetic method of this compound is introduced below.

Step 7: The product from the previous step was dissolved in dry toluene (8mL) under argon. A portion of this stock solution (ImL) was added to a reaction-vial in a Mettler-Toledo Bohdan block using an atmosphere of argon to exclude air. 2-Fluoro-l-iodo-4-methyl-benzene (0.33mmol; prepared from 2-fluoro-4-methyl-phenylamine according to a general literature procedure [S. E. Tunney and J. K. Stille, J. Org. Chem., 52, 748-53 (1987)]) was added as a toluene solution (ImL) followed by 0.5mL of a freshly prepared toluene stock of solution of tris(dibenzylideneacetone)dipalladium(0) (Pd2dba3) and bis[(2-diphenyl- phosphanyl)phenyl] ether DPEphos (corresponding to 0.3 equivalents palladium and 0.6 equivalents DPEphos). Potassium t¡ãt-butoxide (0.66mmol) was added followed by tetra-n- butyl ammonium fluoride (TBAF; 1.0M in THF; 80 microliter). The mixture was stirred at 1000C overnight under argon. Next morning, the volatiles were removed using a Genevac instrument. The residue was dissolved in methanol (4mL) and loaded onto a VacMaster SCX- column (activated with 10% acetic acid in methanol). The product was eluted with acetonitrile. The volatiles were removed in vacuo. The residue was dissolved in methanol (1.5mL) and 4M HCl in diethyl ether (1.5mL) was added. The mixture was shaken at room temperature over the weekend before the volatiles were removed in vacuo. The residue was dissolved in dimethyl sulfoxide (0.18mL) and filtered. A few drops of 20% acetonitrile in water were added, and the mixture was filtered again. The product was isolated by preparative LC/MS as described, concentrated in vacuo, and the product was dissolved in dimethyl sulfoxide (0.78mL) to give a 1OmM solution. LC/MS-data: Method 14, retention time (UV) 2.152 min; UV-purity 79.5%; ELS-purity 100%; mass observed 337.407.

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; H. LUNDBECK A/S; WO2009/76961; (2009); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com