Tag: M.W=400-500

Application of 1402838-08-7, The chemical industry reduces the impact on the environment during synthesis 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde, I believe this compound will play a more active role in future production and life.

Compound 4 (210 mg, 0.51 mmol) was dissolved in 10 mL of anhydrous tetrahydrofuran, 30.5 mg of sodium hydride was added under ice-cooling, and the mixture was warmed to room temperature and stirred for 1 hour. Compound 4a (211 mg, 0.51 mmol) was dissolved in 5 mL of anhydrous tetrahydrofuran in an ice bathAdd to the reaction flask. Warm to room temperature and stir overnight. Quench with saturated ammonium chloride. Add 100 mL water. Use dichloromethane.(50 mL x 3) extraction, and the combined extracts were washed with saturated brine, dried over anhydrous sodium sulfate and evaporated to dryness under reduced pressure. Crude product chromatographyThe product Compound 5 (128 mg, yield 36.0%) was obtained.

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-(1-Trityl-4-imidazolyl)benzaldehyde, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Lunan Pharmaceutical Group Co., Ltd.; Zhang Guimin; (92 pag.)CN107488179; (2017); A;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Some common heterocyclic compound, 124750-92-1, name is Losartan carboxylic acid, molecular formula is C22H21ClN6O2, 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. Quality Control of Losartan carboxylic acid

Step B: 2-butyl-4-chloro-l- { [2 ‘ – (2-trityl-2H-tetrazol-5- yl) biphenyl-4-yl] methyl } -IH-imidazole-5-carboxylic acid To a solution of E3174 (234.58 g, 0.54 mol) in DCM (4500 mL) was added triethylamine (85 mL, 0.59 mol) followed by a solution of trityl chloride (159 g, 0.56 mol) in DCM (800 mL) and the reaction mixture was stirred at rt overnight. The reaction mixture was washed with water, dried (MgSO4), filtered, and concentrated in vacuo. Chromatography over silica eluting with 20-80% acetone/heptane afforded the title compound as an orange solid.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 124750-92-1, its application will become more common.

Reference:
Patent; NICOX S.A.; MERCK & CO. INC.; WO2009/106470; (2009); A2;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Related Products of 1402838-08-7, The chemical industry reduces the impact on the environment during synthesis 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde, I believe this compound will play a more active role in future production and life.

Compound 4 (196 mg, 0.51 mmol) was dissolved in 10 mL of anhydrous tetrahydrofuran, and 30.5 mg of sodium hydride was added on an ice bath, and the mixture was warmed to room temperature and stirred for 1 hour. A solution of compound 4a (211 mg, 0.51 mmol) in 5 mL of anhydrous tetrahydrofuran was added to the reaction flask in an ice bath. The mixture was warmed to room temperature, stirred overnight, quenched with saturated ammonium chloride, added with 100 mL of water and extracted with dichloromethane (50 mL×3). The combined extracts were washed with saturated brine, dried over anhydrous sodium sulfate and evaporated to dryness under reduced pressure. The crude product was purified by column chromatography to give Compound 5 (134 mg, yield 39%).

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-(1-Trityl-4-imidazolyl)benzaldehyde, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Lunan Pharmaceutical Group Co., Ltd.; Zhang Guimin; (92 pag.)CN107488179; (2017); A;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Adding a certain compound to certain chemical reactions, such as: 147403-65-4, name is Methyl 2-ethoxy-1-((2′-(N-hydroxycarbamimidoyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, belongs to imidazoles-derivatives 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 147403-65-4, Recommanded Product: Methyl 2-ethoxy-1-((2′-(N-hydroxycarbamimidoyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate

Example 4Methyl 2-ethoxy- 1 -((2′-(5-oxo-4,5-dihydro- 1 (2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)- 1H- benzo[< ]imidazole-7-carboxylate of formula la l ,8-Diazabicyclo[5.4.0.]undec-7-ene (DBU; 0.1 g, 0.65 mmol) was added dropwise to a mixture of methyl 2-methoxy- l -((2'-((hydroxyamino)iminomethyl)biphenyl-4-yl)methyl)- lH- benzo[i ]imidazole-7-carboxylate (of formula Va; 0.22 g, 0.5 mmol), the corresponding solvent (3 ml) and carbonyldiimidazole (0.1 g, 0.6 mmol) in a reaction vial under stirring and the mixture was stirred at the room temperature for 3 hours. Then, the content of the vial was poured into water ( 10 ml) and, after acidification with acetic acid, the separated solids were aspirated and washed with water. The yields and purity of the products are summarized in Table I. Table I - Yield and purity of the product of Example 4* - Also contains 40.4 % of the starting compound of formula Va; ** - Carbonyl-di- 1 ,2,4- triazole was used instead of carbonyldiimidazole. 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, Methyl 2-ethoxy-1-((2'-(N-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, other downstream synthetic routes, hurry up and to see. Reference:
Patent; ZENTIVA, K.S.; RADL, Stanislav; WO2012/139536; (2012); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Electric Literature of 96797-15-8, 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. 96797-15-8, name is 4-Iodo-1-trityl-1H-imidazole belongs to imidazoles-derivatives compound, it is a common compound, a new synthetic route is introduced below.

A mixture of 4-iodo-1-tritylimidazole (commercially available) (5.0 g, 11.5 mmol) in dichloromethane (50 mL) at -10 C. was treated with ethyl magnesium bromide (3.8 mL, 11.5 mmol, 3M in ether) and allowed to react for 90 m. A solution of 6-methyl-pyridine-2-carbaldehyde (Intermediate D1) (commercially available from Aldrich) (0.93 g, 7.7 mmol) in dichloromethane (10 mL) was added via syringe at -10 C. and stirred for 45 m. The mixture was quenched with water (50 mL) and with a saturated solution of ammonium chloride (60 mL). The residue was isolated in an aqueous workup, extracting with CHCl3 and purified by chromatography on silica gel with 5% NH3-MeOH:CH2Cl2 to give (6-Methyl-pyridin-2-yl)-(1-trityl-1H-imidazol-4-yl)-methanol (Intermediate D2) as a solid, 3.3 g (99%). A solution of (6-methyl-pyridin-2-yl)-(1-trityl-1H-imidazol-4-yl)-methanol (Intermediate D2) (3.7 g, 8.5 mmol) in dioxane (75 mL) was treated with activated manganese(IV) oxide (MnO2), (commercially available from Aldrich): (7 g, 80 mmol) at 90 C. for 20 m. The mixture was filtered through Celite and the solvent was removed under vacuum. The product, (6-methyl-pyridin-2-yl)-(1-trityl-1H-imidazol-4-yl)-methanone (Intermediate D3) was used in the next step without further purification 3.6 g. Methyl triphenylphosphine bromide (commercially available from Aldrich) (2.2 g, 6.16, mmol) in THF(60 mL) at -70 C. was treated with nBuLi (2.44 mL, 2.5M in hexane). The reaction mixture warmed to -50 C. in 1 h. A solution of (6-methyl-pyridin-2-yl)-(1-trityl-1H-imidazol-4-yl)-methanone (Intermediate D3) (1.38 g, 3.2 mmol) in THF (25 mL) was added to the mixture via syringe at -50 C. The mixture was allowed to warm to rt for 1.5 h. The mixture was poured into ether (mL) and washed with water (2×10 mL). The organic solution was dried over MgSO4, filtered and evaporated to leave a residue. This was purified by chromatography on SiO2 with diethyl ether to give 2-methyl-6-[1-(1-trityl-1H-imidazol-4-yl)-vinyl]-pyridine (Intermediate D4) 0.68 g (50%). A mixture of 2-methyl-6-[1-(1-trityl-1H-imidazol-4-yl)-vinyl]-pyridine (Intermediate D4) (460 mg, 1.1 mmol) in trifluoroacetic acid (TFA) (25 mL) was reduced by the action of 10% Pd/C (100 mg) under H2 at 35 psi for 20 h at rt. The mixture was filtered through Celite and freed of solvent under reduced pressure. The residue was purified by chromatography on silica gel with 5% NH3-MeOH:CH2Cl2 to give 2-[1-(1H-imidazol-4-yl)-ethyl]-6-methyl-pyridine (Intermediate D5) as a solid, 150 mg (93%). A mixture of 2-[1-(1H-imidazol-4-yl)-ethyl]-6-methyl-pyridine (Intermediate D5) (150 mg, 0.80 mmol) in THF (8 mL) and water (8 mL) was treated with NaHCO3 (240 mg, 2.86 mmol) and phenylchlorothionoformate (0.35 mL, 2.60 mmol) for 3 h at rt. The mixture was diluted with diethyl ether (35 mL) and water (10 mL). The aqueous layer was removed and extracted with ether (2×10 mL). The organic layers were combined, dried over MgSO4, filtered and concentrated under vacuum. The residue was treated with triethylamine (1 mL) in methanol (9 mL) at rt for 16 h. The solvent was removed and the product was isolated and purified either by tituration with CH2Cl2: hexane or by chromatography on SiO2 with EtOAc or 3 to 7% NH3-MeOH:CH2Cl2. This gave 4-[1-(6-methyl-pyridin-2-yl)-ethyl]-1,3-dihydro-imidazole-2-thione (Compound 9) 50 mg (30%). 1H NMR (300 MHz, DMSO-d6 w/TMS) delta11.9 (s, 1H), 11.7 (s, 1H), 7.60 (t, J=7.5 Hz, 1H), 7.07 (d, J=7.5 Hz, 1H), 7.02 (d, J=7.5 Hz, 1H), 6.53 (s, 1H), 3.95 (q, J=6.9 Hz, 1H), 2.42 (s, 3H), 1.46 (d, J=7.2 Hz, 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, 4-Iodo-1-trityl-1H-imidazole, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Allergan, Inc.; US2006/69143; (2006); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Application of 1402838-08-7, 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. 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde belongs to imidazoles-derivatives compound, it is a common compound, a new synthetic route is introduced below.

1-(2-chlorobenzofuran-5-yl)ethane-1-one (0506-157) (120 g, 0.61 mmol, 1.0 equiv) and2-(1-trityl-1H-imidazol-4-yl)benzaldehyde (0105-1) (380 mg, 0.92 mmol, 1.5 equiv)Dissolved in 10 ml dioxaneAdd 1 ml concentrated sulfuric acid dropwise to the ice bath.The temperature was raised to 90C and the reaction was stirred for 18 hours.Cool to room temperature and add dropwise to ice water. Under ice bath, add sodium hydroxide to adjust pH>8, extract with ethyl acetate, separate, spin dry, and purify the crude product with silica gel column chromatography (eluent: Dichloromethane/methanol = 200/1 to 40/1) gives the product1-(2-Chlorobenzofuran-5-yl)-2-(5H-imidazo[5,1-a]isoindoline-5-yl)ethane-1-one (100 mg, 46.5%) .

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-(1-Trityl-4-imidazolyl)benzaldehyde, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Guangzhou Bi Beite Pharmaceutical Co., Ltd.; Cai Xiong; Qian Changgeng; Weng Yunwo; Qing Yuanhui; Liu Bin; Lin Mingsheng; Wang Yanyan; (126 pag.)CN107383024; (2017); A;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

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. 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde, A new synthetic method of this compound is introduced below., HPLC of Formula: C29H22N2O

2-(1-trityl-1H-imidazol-4-yl)benzaldehyde (0105-1) (250 mg, 0.6 mmol, 1.0 equiv),Compound (dimethyl 2-(isoquinolin-6-yl)-2-oxoethyl)phosphate (0803-127) (400 mg, 1.4 mmol, 2.3 eq.)And cesium carbonate (391 mg, 1.2 mmol, 2.0 equiv)Mixed in isopropyl alcohol (30 ml),The reaction was stirred at room temperature overnight.After the reaction is completed, quench with water, extraction with dichloromethane, anhydrous sulfur in the organic phaseThe sodium sulfate was dried and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (eluent: dichloromethane/methanol=100/1-50/1) to give a product.1-(isoquinolin-6-yl)-3-(2-(1-trityl-1H-imidazol-4-yl)phenyl)prop-2-en-1-one (300 mg, Rate: 87%).

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; Guangzhou Bi Beite Pharmaceutical Co., Ltd.; Cai Xiong; Qian Changgeng; Weng Yunwo; Qing Yuanhui; Liu Bin; Lin Mingsheng; Wang Yanyan; (126 pag.)CN107383024; (2017); A;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

These common heterocyclic compound, 124750-92-1, name is Losartan carboxylic 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. Recommanded Product: 124750-92-1

Step B: To the dichloromethane solution of step A product was added triethylamine followed by the addition of triphenylmethyl chloride in methylene chloride and the resulting reaction mixture was stirred at room temperature. The reaction mixture was triturated with water, dried over magnesium sulfate, filtered, concentrated in vacuo, loaded on a silica gel column and eluted with 20-80% acetone / n-hexane to give2-Butyl-4-chloro-1 – {[2 ‘- (2-trityl-2H-tetrazolyl-5) biphenyl-4-] methyl} -1H-imidazole- carboxylic acid.

The synthetic route of Losartan carboxylic acid has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Zhejiang Yongtai Technology Co., Ltd.; Lin, Jiaohua; He, Renbao; (22 pag.)CN104447899; (2017); B;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

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 1403474-70-3 as follows. Application In Synthesis of Ethyl 2-ethoxy-1-((2′-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1′-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate

Example 2 Preparation of the product 2-Ethoxy-3- [2 ‘- (5-oxo-4,5-dihydro- [1,2,4] oxadiazol-3-yl) 4-ylmethyl] -3H-benzimidazole-4-carboxylate 55.1 g,0.4 MN NaOH into the reaction bottle,75 C stirring reaction to the raw material reaction is completed. The reaction solution was cooled to room temperature. The filtrate was added with 820ml of absolute ethanol, filtered and kept at 20 C. The pH was adjusted to 1 with 2M HC1 solution. A large amount of solid was precipitated, stirred for 1 hour, filtered and washed with water. 50.6 g,HPL (^ i ^ S 98.6%

According to the analysis of related databases, 1403474-70-3, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Hunan Xianjin Xiangjiang Pharmaceutical co., LTD; YUAN, XIUJU; YAO, LIANGYUAN; ZONG, AIJUN; DENG, MENGRU; (12 pag.)CN103664921; (2016); B;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Electric Literature of 124750-92-1, 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 124750-92-1 as follows.

460 grams of free acid was dissolved in 5 liters of acetic acid, glacial. The solution was filtered through a glass frit. The filtrate was added to 6 liters of 1.1 N HCl in acetic acid, glacial over 1 hour. Crystallization began just prior to the end of filtrate addition, and the resulting material was aged for 1 hour. An ice and water bath was added to cool the batch, and the batch was aged 1 hour. 12.5 liters of isopropyl acetate was added over 1 hour, and the resulting material was aged at 3-4C for 1 hour.Resulting material was filtered and washed with 1 liter isopropyl acetate displacement wash, 2 x 1 liter isopropyl acetate slurry wash, and 2.5 liter isopropyl acetate displacement wash. Resulting material was air dried 45 minutes, then dried by pulling nitrogen through filter cake overnight followed by drying at 350C in a vacuum oven until constant weight. The resulting hydrochloric acid salt was 2-butyl~4-chloro- l-[(2′-(l-H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I. The solid was then analyzed by X-ray Powder Diffraction. The diffractogram for 2-butyl-4-chloro-l-[(2′-(l- H-tetrazol-5-yl)biphenyl-4-yl)methyl]-imidazole-5-carboxylic acid hydrochloride Form I is characterized by principal d-spacings of 12.96, 4.75, 3.97, 3.79, 3.77, 3.71, and 3.44A, more specifically 12.96, 8.32, 8.13, 7.06, 5.18, 4.75, 4.64, 4.45, 4.41, 4.33, 4.19, 3.97, 3.86, 3.79, 3.77, 3.71, 3.59, 3.44, 3.15, and 2.92A.

According to the analysis of related databases, 124750-92-1, the application of this compound in the production field has become more and more popular.

Reference:
Patent; MERCK & CO., INC.; WO2006/115834; (2006); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem