Tag: M.W=400-500

Related Products of 147403-65-4,Some common heterocyclic compound, 147403-65-4, name is Methyl 2-ethoxy-1-((2′-(N-hydroxycarbamimidoyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, molecular formula is C25H24N4O4, 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 122-Ethoxy- 1 -((2′-(5-oxo-4,5-dihydro- 1 ,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)- 1H- benzo[( ]imidazole-7-carboxylic acid – azilsartan of formula IIA solution of ethyl chloroformate (2.7 g, 24.9 mmol) in dry DMF was added dropwise to a mixture of methyl 2-ethoxy-l -((2′-((hydroxyamino)iminomethyl)biphenyl-4-yl)methyl)-l H- benzo[i ]imidazole-7-carboxylate (of formula Va; 10.6 g, 23.8 mmol), dry DMF (75 ml) and pyridine (2.25 g)under stirring in an ice-cold bath under nitrogen and the mixture was stirred under cooling under nitrogen for 6 hours. The reaction mixture was poured into a separation funnel containing water (150 ml) and the mixture was extracted with ethyl acetate (5 x 100 ml). The extract was dried with MgS04 and, after evaporation, 12.7 g of a solid yellowish substance were obtained. The evaporation residue was dissolved in DMSO (200 ml) and t- BuOK (8 g, 71.3 mmol) was added under stirring and cooling and the mixture was stirred at the room temperature for 5 h. Then, the reaction mixture was poured into water (750 ml) and the resulting solution was acidified with 5 % HCl. The separated product was aspirated, washed with water and air-dried. 1 1.2 g (the quantitative yield would be ca. 10.9 g) of a product containing 88.3 % of azilsartan of formula II according to HPLC was obtained. Crystallization from isopropanol provided 9.3 g (85.5%) of azilsartan of formula II with the HPLC content of 98.7% with the melting point of 205 to 208 C.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route Methyl 2-ethoxy-1-((2′-(N-hydroxycarbamimidoyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, its application will become more common.

Reference:
Patent; ZENTIVA, K.S.; RADL, Stanislav; STACH, Jan; WO2012/139535; (2012); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Related Products of 147403-65-4, A common heterocyclic compound, 147403-65-4, name is Methyl 2-ethoxy-1-((2′-(N-hydroxycarbamimidoyl)-[1,1′-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, molecular formula is C25H24N4O4, 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.

Example 2 Methyl 2-ethoxy- 1 -((2′-((hydroxyamino)iminomethyl)biphenyl-4-yl)methyl)- 1 H-benzo [d] – imidazole-7-carboxylate (la) – modification of the process (US 5,583,141 ; EP 0,520,423)The product obtained using the method of Example 1 (3.9 g) was dissolved in dichloromethane (400 ml) and the resulting, still turbid solution was washed with 4 x 50 ml of 5 % HC1. Thus obtained aqueous solution was alkalinized with a concentrated (20 %) solution of sodium hydroxide and the resulting precipitate was aspirated and washed with water. After drying 1.6 g (the total yield of Example 1 and Example 2 is 36.0 %) of the substance (la) were obtained, containing, according to HPLC, 96.7 % of the product (la), an undetectable amount of the starting nitrile (IVa) and 1.3 % of the desethyl nitrile (Via).

The synthetic route of 147403-65-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ZENTIVA, K.S.; RADL, Stanislav; WO2012/119573; (2012); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Adding a certain compound to certain chemical reactions, such as: 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde, 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 1402838-08-7, Recommanded Product: 2-(1-Trityl-4-imidazolyl)benzaldehyde

A slurry of tert-butyll-oxo-7-azaspiro [3.5jnonane-7-carboxylate (2.27 g, 9.49 mmol), 2-[1-(triphenylmethyi)-l H-imidazol-4-yl]benzaldehyde (4.04 g, 9.74 mnioi) and Ca(OH)2 (2.10 g, 28.33 mmol) in EtOH (100 mL) were mixed and stirred overnight at 80 C. The solids were filtered out. The resulting mixture was concentrated under vacuum. This resulted in 7.4 g (crude) of tert-butyl(2E)-1 -oxo-2-([2-[ I -(tripbenylmethyl)-IN-imidazol-4-yI] phenyljmethylidene)-7- azaspiro[3.5]nonane-7-crboxy1ate as a yellow solid. LCMS (ESI) rniz 636.2 [M+HJ

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-(1-Trityl-4-imidazolyl)benzaldehyde, and friends who are interested can also refer to it.

Reference:
Patent; GENENTECH, INC.; PEI, Zhonghua; PASTOR, Richard; GAZZARD, Lewis; PARR, Brendan; LIU, Wendy; MENDONCA, Rohan; WU, Guosheng; YUEN, Po-Wai; (183 pag.)WO2019/5559; (2019); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Adding a certain compound to certain chemical reactions, such as: 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde, 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 1402838-08-7, category: imidazoles-derivatives

1-(2-Hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)ethyl-1-one (100 mg, 0.46 mmol),2-(1-Triphenylmethyl-1H-imidazol-4-yl)benzaldehyde (190 mg, 0.46 mmol) was dissolved in tetrahydrofuran (4.0 mL).The sodium ethoxide solution (31 mg, 21%/wt%) was added dropwise and stirred at room temperature overnight.After TLC monitoring, the reaction was completed, the solvent was evaporated under reduced pressure, and saturated ammonium chloride solution (10 mL) was added.Extracted with dichloromethane (20 mL), and the organic phase was evaporated to dryness.The residue was used directly in the next step.The residue obtained above was dissolved in a mixed solution of methanol (4 mL) and acetic acid (1 mL).After reacting at 90 C for 3 h, TLC detected the reaction completely.The solvent was evaporated under reduced pressure and the residue was purified by flash column chromatography.Obtained the target Compound114mg,The yield was 72%.

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; Suzhou Guokuang Pharmaceutical Technology Co., Ltd.; Hangzhou Anuo Bio-pharmaceutical Technology Co., Ltd.; Mei Desheng; Lu Yang; Yang Donghui; Li Pan; (50 pag.)CN108424415; (2018); 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. 96797-15-8, name is 4-Iodo-1-trityl-1H-imidazole, A new synthetic method of this compound is introduced below., name: 4-Iodo-1-trityl-1H-imidazole

To a solution of 4-IODO-L-TRITYL-LH-IMIDAZOLE (1 eq) in THF at room temperature was added ethylmagnesium bromide (1.2 eq) under dry conditions. After stirring for 90 minutes, zinc chloride (1.2 eq) was added to the reaction mixture. After stirring for another 90 minutes, tetrakis (triphenylphosphine) palladium (10%) and 5- bromo-2-methylpyridine (1.2 eq) were added to the reaction mixture. Following that, the reaction mixture was heated in a 70C oil bath overnight. Upon cooling, the reaction was diluted with dichloromethane and washed with a EDTA buffer (at approximately pH 9), NaCl, dried over sodium sulfate, filtered and concentrated. The crude product was disolved in ethanol and concentrated HCl was added to the solution at room temperature. The reaction mixture was heated in a 50C oil bath for 2 hours. Upon cooling, the reaction was filtered and washed with ethyl ether to yield 5- (1H- imidazol-4-yl) -2-methyl-pyridine (63%). MH+ (160)

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; CHIRON CORPORATION; WO2004/96822; (2004); A2;,
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 suspensionof 4 (3.0 g, 6.9 mmol), the appropriate 2-formyl boronic acid(1.6 g, 10.7 mmol) and K3PO4 (4.4 g, 20.8 mmol) in DMF (30 mL) andwater (6 mL) was purged with nitrogen for 5 min, followed by theaddition of Pd(PPh3)4 (0.6 g, 0.5 mmol) and the mixturewas purgedwith nitrogen for another 5 min. The reaction mixture was stirredat 90 C for 16 h under an atmosphere of N2. The solution wasallowed to cool and was filtered through a plug of celite. Themixture was diluted with water (50 mL) and was extracted withethyl acetate to afford the crude product which was purified byflash column chromatography on silica gel to yield 6 as a white solid(1.9 g, 66.7%). Mp 147e149 C. 1H NMR (300 MHz, Chloroform-d)d(ppm) 7.97 (dd, J 7.8, 1.4 Hz, 1H), 7.72e7.54 (m, 3H), 7.38 (h,J 3.2 Hz,11H), 7.25e7.19 (m, 6H), 7.07 (d, J 1.3 Hz, 1H). MS (EI) m/z 415.2 [MH].

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:
Article; Zou, Yi; Wang, Fang; Wang, Yan; Sun, Qirui; Hu, Yue; Li, Yuezhen; Liu, Wen; Guo, Wenjie; Huang, Zhangjian; Zhang, Yihua; Xu, Qiang; Lai, Yisheng; European Journal of Medicinal Chemistry; vol. 140; (2017); p. 293 – 304;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Electric Literature of 96797-15-8, 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 96797-15-8 as follows.

To a solution of 4-IODO-1-TRITYL-LH-IMIDAZOLE (A) (1 eq) in THF at room temperature was added ethylmagnesium bromide (1.2 eq) under dry conditions. After stirring for 90 minutes, zinc chloride (1.2 eq) was added to the reaction mixture. After stirring for another 90 minutes, tetrakis (triphenylphosphine) palladium (10%) and 5-bromo-2-methoxypyridine (1.2 eq) were added to the reaction mixture. Upon cooling, the reaction was diluted with dichloromethane and washed with a EDTA buffer (at approximate pH 9), NACI (sat. ), dried over sodium sulfate, filtered, and concentrated. MH+ (418)

According to the analysis of related databases, 96797-15-8, the application of this compound in the production field has become more and more popular.

Reference:
Patent; CHIRON CORPORATION; WO2004/96822; (2004); A2;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Adding a certain compound to certain chemical reactions, such as: 96797-15-8, name is 4-Iodo-1-trityl-1H-imidazole, 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 96797-15-8, category: imidazoles-derivatives

[270] To a solution of (2-forrnylphenyl)boronic acid (2.0 g, 13.3 rnrnol) in a rnixed solvent of N,N- dirnethylforrnarnide (DMF) (60 rnL) and water (12 rnL) was successively added 4-iodo-1- trityl-1H-irnidazole (6.1 g, 14.0 rnrnol), and potassiurn phosphate (5.6 g, 26.6 rnrnol). After degassing with nitrogen, the resulted rnixture was added tetrakis(triphenylphosphine)palladiurn(0) (Pd(PPh3)4) (300 rng, 0.26 rnrnol). The resulted rnixture was degassed with nitrogen and stirred at 90C for overnight under nitrogen. And then the rnixture was cooled down to roorn ternperature and filtered, the filtrate was added water (60 rnL), extracted with ethyl acetate (100 rnLx2). The cornbined organic phase was washed with brine (25 rnL), dried over sodiurn sulfate, filtered and concentrated. The residue was purifiedby colurnn chrornatography on silica gel (petroleurn ether: ethyl acetate= 6:1) to afford cornpound 1.1 (3.3 g, yield: 60%) as a white solid.[271] rn/z: [M+H]415

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; SHANGHAI DE NOVO PHARMATECH CO.,LTD.; LI, Qun; GAO, Daxin; (158 pag.)WO2016/131380; (2016); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Related Products of 1402838-08-7, 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. 1402838-08-7, name is 2-(1-Trityl-4-imidazolyl)benzaldehyde, This compound has unique chemical properties. The synthetic route is as follows.

2-(1-trityl-1H-imidazol-5-yl)benzaldehyde (0105-1) (200 mg, 0.483 mmol, 1 eq),Compound ((5-(2-(dimethoxyphosphoryl)acetyl)benzofuran-2-yl)methyl) tert-butyl carbonate (0207-50) (211 mg, 0.531 mmol, 1.1 eq.) withCesium carbonate (314 mg, 0.966 mmol, 2 eq)Mixed in isopropanol (10 ml),The mixture was stirred at room temperature for 16 hours.After the reaction was completed, quenched with water and filtered to give the target product (305 mg, yield: 92.14%) as a yellow solid.

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

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, 96797-15-8, name is 4-Iodo-1-trityl-1H-imidazole, 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. Product Details of 96797-15-8

Compound 1 (2.2 g, 5.0mmol), o-formylphenylboronic acid(1.2 g, 7.5mmol), K3PO4 (3.2 g, 15mmol), Pd (PPh3)4 (0.6 g, 1.0mmol) is dissolved in DMF/H20 (30mL/6mL). The system is replaced with nitrogen and warmed at 90C, the reaction is stirred overnight. The reaction solution is diluted with ethyl acetate (50mL), wash with saturated brine (25mL X 3), dry over anhydrous sodium sulfate, and dry under reduced pressure. Crude column chromatography (PE: EA = 5:1), and then obtained brown solid compound 2 (810 mg, 39%).

The synthetic route of 4-Iodo-1-trityl-1H-imidazole has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Lunan Pharmaceutical Group Co., Ltd.; Zhang Guimin; Guan Yongxia; Li Xin; (15 pag.)CN107556315; (2018); A;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem