Tag: M.W=200-300

Some common heterocyclic compound, 20555-91-3, name is 1,2-Dichloro-4-iodobenzene, molecular formula is C6H3Cl2I, 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: 20555-91-3

EXAMPLE 32 (3R,4S)-4-(3′,4′-Dichlorobiphenyl-4-yloxy)-1-pyridin-3-yl-pentan-3-ol oxalic acid salt Prepared according to the method described in Example 12b) from 3,4-dichloro-iodobenzene (0.273 g), ethanol (2 ml), toluene (5 ml), 2M aqueous sodium carbonate (0.5 ml), (1S,2R)-4-[2-(tert-butyldimethylsilanyloxy)-1-methyl-4-pyridin-3-ylbutoxy]benzeneboronic acid (0.2 g, Example 11)), and tetrakis(triphenylphosphine)palladium (0) (0.025 g) with heating at 120 C. for 4 hours. After work-up, the residue was purified by normal-phase HPLC eluding a gradient of 0-25% ethanol in dichloromethane to give the title compound which was converted to the oxalic acid salt by treatment with a saturated ethereal solution of oxalic acid to give the title compound as a solid (0.229 g). m.p. 86-88 C. MS (APCI) 402, 404 (M+H)+ 1H NMR (DMSO) 8.46(1H, d); 8.44 (1H, d); 7.87 (1H, d); 7.70 (1H, dt); 7.65-7.58 (4H, m); 7.35 (1H, dd); 7.0 (2H, d); 4.35 (1H, dq); 3.60-3.52 (1H, m); 2.88-2.78 (1H, m) 2.61 (1H, m); 1.95-1.82 (1H, m); 1.70-1.59 (1H, m); 1.25 (3H, d).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 20555-91-3, its application will become more common.

Reference:
Patent; AstraZeneca AB; US6300352; (2001); B1;,
Iodide – Wikipedia,
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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. 25309-64-2, name is 1-Ethyl-4-iodobenzene belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 25309-64-2

General procedure: To a stirred solution of aryl halides (1.0 mmol) and indoline/indoline carboxylic acid (1.0 equiv) in dry DMSO (2.0 mL) at rt was added nano CuO (5.0 mol %) followed by Cs2CO3 (2.0 equiv) and heated at 80 C for 8 h. The progress of the reaction was monitored by TLC. After the reaction was complete, the reaction mixture was cooled to room temperature and catalyst was filtered, the crude residue was extracted with ethyl acetate (3 ¡Á 10 mL). The combined organic layers were extracted with water, saturated brine solution, and dried over anhydrous Na2SO4. The organic layers were evaporated under reduced pressure and the resulting crude product was purified by column chromatography by using ethyl acetate/hexane (7:3) as eluent to give the corresponding N-substituted indoles in excellent yields. The identity and purity of the product were confirmed by 1H, 13C NMR, and mass spectra.

The synthetic route of 25309-64-2 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Reddy, K. Harsha Vardhan; Satish; Ramesh; Karnakar; Nageswar; Tetrahedron Letters; vol. 53; 24; (2012); p. 3061 – 3065;,
Iodide – Wikipedia,
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34883-46-0, name is 1-Iodo-2-phenoxybenzene, 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. Computed Properties of C12H9IO

(1): To 1-iodo-2-phenoxybenzene (2 g, 6.8 mmol)a solution of triethylamine (20 mL) added to phenylacetylene(0.83 g, 8.1 mmol), Pd(PPh3)2Cl2 (95 mg, 135 mumol), CuI (26 mg, 135 mumol).Under argon protection conditions, after 10 hours of reaction,Triethylamine was removed under reduced pressure.The residue was extracted with ethyl acetate (20 mL¡Á3).Then washed twice with water (10 mL) and saturated brine (10 mL).Dry over anhydrous sodium sulfate, filter, and remove the solvent under pressure.The residue was purified by silica gel column chromatography eluting elut1-phenoxy-2-(phenylethynyl)benzene(1.6 g, 88% yield).

The synthetic route of 34883-46-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Zhongshan University Tumor Cure Center (Zhongshan University Affiliated Tumor Hospital ? Zhongshan University Tumor Institute); Wen Shijun; Huang Peng; Zhu Daqian; Tu Yalin; Luo Bingling; (28 pag.)CN108976248; (2018); A;,
Iodide – Wikipedia,
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Reference of 156150-67-3,Some common heterocyclic compound, 156150-67-3, name is 2-Chloro-1-fluoro-4-iodobenzene, molecular formula is C6H3ClFI, 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 22 : 5-([l ,2,4] triazolo [1 ,5-a] pyridin-6-yl)-4-(3-chloro-4-fluorophenyl)-2,2- dimethylfuran-3(2H)-one; [00195] Cesium acetate (167 mg, 0.000872 mol) was added to a round bottom flask and dried under vacuum at 125 C for 2 hours. Palladium acetate (0.98 mg, 0.0000044 mol), tris(4-trifluoromethylphenyl)phosphine (8.1 mg, 0.000017 mol), and N,N- dimethylformamide (1.7 mL, 0.022 mol) were added to the dried cesium acetate and the mixture stirred for 30 min. 5-([l,2,4]triazolo[l,5-a]pyridin-6-yl)-2,2-dimethylfuran-3(2H)- one (100.0 mg, 0.0004362 mol) and 2-chloro-l-fluoro-4-iodobenzene (112 mg, 0.000436 mol) in N,N-dimethylformamide (1.7 mL, 0.022 mol) were added and the mixture stirred at 125 0C for 18 hr. The mixture was partitioned between ethyl acetate and water. The organic phase was washed with brine, dried over sodium sulfate, filtered, and concentrated to give a yellow oil. The yellow oil was purified on HPLC eluting with acetonitrile: water (0.1% TFA) to give 20.0 mg (12.8%) of the title compound as a yellow solid.1H NMR (300 MHz, Methanol-^) delta 9.19 (s, IH), 8.49 (s, IH), 7.75 (m, 3H), 7.29 (m, 2H), 1.59 (s, 6H). MS (ESP+) m/z 358.09.

The synthetic route of 156150-67-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BIOGEN IDEC MA INC.; WO2008/94574; (2008); A2;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Reference of 619-58-9, 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. 619-58-9, name is 4-Iodobenzoic acid belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

Method B.A solution of 4-methoxyphenyl boronic acid (1 g, 6.58 mmol), 4-iodobenzoic acid (1.63 g, 6.58 mmol) and cesium carbonate (5.36 g, 16.45 mmol) in 3:1 1,2- dimethoxyethane/water was deoxygenated with nitrogen for 15 minutes. Pd(PPtLs)4 (380 mg, 0.329 mmol) was then added and the solution was heated to 80 C for 6h. The reaction was allowed to cool and acidified with 2M HCl which caused a precipitate to form. The precipitate was filtered and the filtrate was extracted twice with dichloromethane. The organic layer was then dried over magnesium sulfate, filtered through diatomaceous earth filter aid (CELITE) and evaporated under reduced pressure to yield a combined 1.5O g (95%). 1HNMR (DMSO): delta 7.99 (d, J=8.4 Hz, 2H), 7.74 (d, J=8.4 Hz, 2H), 7.69 (d, J=8.7 Hz, 2H), 7.04 (d, J=8.7 Hz, 2H), 3.80 (s, 3H). 13CNMR (DMSO): delta 167.17, 159.49, 143.90, 131.16, 129.91, 128.77, 128.09, 126.08, 114.45, 55.17.

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

Reference:
Patent; GEORGETOWN UNIVERSITY; WO2009/146013; (2009); 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. 618-91-7, name is Methyl 3-iodobenzoate, A new synthetic method of this compound is introduced below., Application In Synthesis of Methyl 3-iodobenzoate

General procedure: A mixture ofmethyl 3-iodobenzoate (1 mmol), corresponding amine (3 mmol), K2CO3(4 mmol), CuI (0.2 mmol) and L-proline (0.4 mmol) in 15 mL of DMSO was heatedat 60 C for 8 h. The cooled mixture was pour into 150 ml water, and extractedwith ethyl acetate (3 ¡Á 15 mL), the organic fractions were combined, washedwith saturated brine (2 ¡Á 15 ml) prior to drying over anhydrous sodium sulfate.After filtration and concentrate using a rotary evaporator, the residue was purified by silica gel column chromatographyusing a mixture of petroleum ether/ethyl acetate (20 : 1, v/v) as eluent toafford the desired product.

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:
Article; Li, Zheng; Pan, Miaobo; Su, Xin; Dai, Yuxuan; Fu, Mian; Cai, Xingguang; Shi, Wei; Huang, Wenlong; Qian, Hai; Bioorganic and Medicinal Chemistry; vol. 24; 9; (2016); p. 1981 – 1987;,
Iodide – Wikipedia,
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Related Products of 699016-40-5, 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. 699016-40-5, name is 2-Fluoro-4-iodobenzaldehyde, This compound has unique chemical properties. The synthetic route is as follows.

Step 1-B: To a solution of 2-fluoro-4-iodo-benzaldehyde (17.40 g, 69.60 mmol) in anhydrous tetrahydrofuran (300 mL) at -10 C. under an atmosphere of nitrogen was added 3.0 M methylmagnesium chloride in tetrahydrofuran (27.84 mL, 83.52 mmol) via syringe at such a rate as to maintain the temperature of the reaction mixture below 0 C. The reaction was stirred for 30 minutes while warming to room temperature. Saturated aqueous ammonium chloride solution was added and the mixture was diluted with ethyl acetate (200 mL). The organic layer was separated and the aqueous layer was extracted with ethyl acetate (2*50 mL). The organic extracts were combined, washed with water (1*50 mL), brine, dried over sodium sulfate, filtered and concentrated in vacuo. The crude product was purified by chromatography over silica gel gradient eluted with 15 to 40% v/v ethyl acetate/hexanes to give 1-(2-fluoro-4-iodo-phenyl)-ethanol (15.50 g, 84%).

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

Reference:
Patent; Chen, Shaoqing; Huby, Nicholas J.S.; Kong, Norman; Moliterni, Jonh Anthony; Morales, Omar Jose; US2009/170920; (2009); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Adding a certain compound to certain chemical reactions, such as: 18698-96-9, name is 2-(2-Iodophenyl)acetic 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 18698-96-9, category: iodides-buliding-blocks

2-(2-Iodophenyl)acetamide (107-2). HATU (50.8 g, 134 mmol) was added to a stirred solution of 107-1 (28 g, 107 mmol), NH3 (321 ml, 160 mmol, 0.5 M/dioxane), iV-methylmorpholine (23.5 ml, 214 mmol) in . DMF (300 ml). The mixture was stirred for 16 hours and then was diluted with EtOAc and washed with H2O, sat NaHCO3, brine, dried over anhydrous MgSO4, filtered and 2/3 solvent was removed in vacuo. The solid was collected, washed with diethyl ether and dried in vacuo to afford 29-2 11.2g, 40.2percent) as a white solid.1H NMR (500 MHz, CDCl3) delta7.i (d, 1 H, J = 8 Hz), 7.36 (m, 2 H), 7.00 (m, 1 H), 5.38 (s, 2 H), 3.75 (s, 2H).

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; MERCK & CO., INC.; WO2008/51532; (2008); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Application of 2265-93-2, 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. 2265-93-2, name is 2,4-Difluoroiodobenzene, This compound has unique chemical properties. The synthetic route is as follows.

A mixture of (3S)-piperidin-3-ol hydrochloride (0.50 g, 0.0036 mol), l,3-difl’uoro-4- iodobenzene (0.522 mL, 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 without further purifications (529 mg, 69%). LCMS (M+H): 214.2.

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

Reference:
Patent; INCYTE CORPORATION; WO2007/89683; (2007); 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. 103962-05-6, name is 1-Iodo-4-(trifluoromethoxy)benzene, This compound has unique chemical properties. The synthetic route is as follows., Application In Synthesis of 1-Iodo-4-(trifluoromethoxy)benzene

Example 59. Preparation of 3-bromo-l-(4-(trifluoromethoxy)phenyl)-lH-l,2,4-triazole (B61) To a 250 mL reaction flask was added 3-bromo-lH-l,2,4-triazole (5 g, 33.8 mmol), copper(I) iodide (0.644 g, 3.38 mmol) and cesium carbonate (11.01 g, 33.8 mmol). The flask was evacuated/backfilled with N2, then DMSO (33.8 ml) and l-iodo-4-(trifluoromethoxy)benzene (4.87 g, 16.90 mmol) were added. The reaction mixture was heated to 100 ¡ãC for 20 h. The reaction was cooled to room temperature, diluted with EtOAc and filtered through a plug of Celite. The Celite was further washed with EtOAc. Water was added to the combined organics, and the layers were separated. The aqueous phase was neutralized to pH 7, and further extracted with EtOAc. The combined organics were concentrated in vacuo. Purification via flash chromatography (silica/EtO Ac/Hex) yielded 3-bromo-l-(4- (trifluoromethoxy)phenyl)-lH-l,2,4-triazole as an off white solid (3.78 g, 12.27 mmol, 72.6percent): mp 69-70 ¡ãC; ]H NMR (400 MHz, CDC13) delta 8.44 (s, 1H), 7.70 (d, / = 8.9 Hz, 2H), 7.38 (d, J = 8.5 Hz, 2H); 19F NMR (376 MHz, CDC13) delta -58.04; EIMS m/z 307.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 103962-05-6.

Reference:
Patent; DOW AGROSCIENCES LLC; CROUSE, Gary D.; DEMETER, David A.; SPARKS, Thomas C.; WANG, Nick X.; DENT, William Hunter; DEAMICIS, Carl; NIYAZ, Noormohamed M.; BAUM, Erich W.; FISCHER, Lindsey G.; GIAMPIETRO, Natalie C.; FRITZ, Amanda E.; WO2014/11429; (2014); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com