Category: 486460-21-3

Adding a certain compound to certain chemical reactions, such as: 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, belongs to pyrazines 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 486460-21-3, Application In Synthesis of 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

Potassium tert-butoxide (2.24 g, 20 mmol) was dissolved in 40 mL of tetrahydrofuran in a 100 mL single-necked flask.Stir at room temperature for one minute. Then compound III (1.91 g, 10 mmol) was added in sequence.Compound II (2.60 g, 10 mmol) was stirred at room temperature for 60 min.Thereafter, the reaction solvent tetrahydrofuran was distilled off under reduced pressure, and then 50 mL of water and 50 mL of dichloromethane were added.The organic phase was extracted and the organic phase was dried with anhydrous sodium sulfate and evaporatedThe crude product was recrystallized from dichloromethane and cyclohexane to give 3.33 g of Compound IV.The yield was 82% and the purity was 99%.

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, 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Anqing Qichuang Pharmaceutical Co., Ltd.; Wu Xueping; Xing Jigang; Yan Dongyang; Chen Yao; (11 pag.)CN108178761; (2018); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Reference of 486460-21-3,Some common heterocyclic compound, 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, molecular formula is C6H7F3N4, 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.

phosgene(725 mg, 9.2 mmol) and 1- (2,3-bis (4-fluorophenoxy) benzoic acid methyl ester in the presence of methylene chloride, 6-nitrophenyl) piperazine crude (1.213g, 5.0mmol) in the mixture, the temperature below 0 C, 10min added, maintained at 0 C reaction lh, the direct response to the next step . To the above reaction solution was added 3- (trifluoromethyl) -5,6,7,8-tetrahydro- [1,2,4] triazolo [4,3-a] pyrazine (800 mg, And triethylamine (842 mg, 8.4 mmol). The temperature of the reaction system was raised to room temperature and stirred for 20 h. The reaction was quenched by the addition of 20 ml of saturated sodium bicarbonate solution and extracted with dichloromethane (20 ml of X2). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, concentrated and purified by column chromatography (petroleum ether: ethyl acetate = 3: 2) Yellow solid 1.345 g, 52.1% yield in three steps.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, its application will become more common.

Reference:
Patent; Shanghai Institute Of Pharmaceutical Industry; China State Institute of Pharmaceutical Industry; Meng, Xiangguo; Cai, Zhengyan; Zhou, Weicheng; Jiang, Jingzhang; Zhu, Yijun; Ge, Yuanyuan; Yan, Pingping; (32 pag.)CN103172635; (2016); B;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Adding a certain compound to certain chemical reactions, such as: 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, belongs to pyrazines 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 486460-21-3, Recommanded Product: 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

Example 1 : Preparation of (S)-benzyl 1-hydroxy-4-oxo-4-(3-(trifluoromethyl)- 5,6-dihydro-ri ,2,41triazolor4,3-aipyrazin-7(8H)-yl)butan-2-ylcarbamate A 2.0 M solution of AIMe3 in hexanes (0.98 ml_, 1.96 mmol) was added to a solution of 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1 ,2,4]triazolo[4,3-a]pyrazine (271 mg, 1.41 mmol) in anhydrous methylene chloride (5 ml_). The resulting mixture was added dropwise to a solution of (S)-benzyl 5-oxotetrahydrofuran- 3-ylcarbamate (265 mg, 1.13 mmol) in anhydrous methylene chloride (5 ml_) at 0 0C. When the reaction was completed, 1 M KHSO4 solution (25 ml_) was added slowly. The layers were separated and the aqueous layer was extracted with methylene chloride (25 ml_). The organic layers were mixed, dried over anhydrous Na2SO4, filtered and concentrated to dryness to yield (S)-benzyl 1 -hydroxy-4-oxo-4-(3-(trifluoromethyl)-5,6-dihydro- [1 ,2,4]triazolo[4,3-a] pyrazin-7(8H)-yl)butan-2-ylcarbamate (353 mg, 0.83 mmol, 73% yield).

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, 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; ESTEVE QUIMICA, S.A.; BARTRA SANMARTI, Marti; RUSTULLET OLIVER, Albert; FERNANDEZ HERNANDEZ, Sara; MONSALVATJE LLAGOSTERA, Montserrat; WO2010/97420; (2010); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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. 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, This compound has unique chemical properties. The synthetic route is as follows., COA of Formula: C6H7F3N4

General procedure: Nucleophilic reagent (2 mmol), trimethylamine (5 mmol) and S3(2 mmol) were dissolved in N,N-dimethylformamide (2 mL) at 0 C.The reaction mixture was stirred for 2e10 h, poured into water(10 mL), and extracted by ethyl acetate (30 mL) in two times. Thecombined organic layer was washed by saturated brine andconcentrated to give the crude residue, which was purified byrecrystallization or flash chromatography.

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 486460-21-3.

Reference:
Article; Xing, Jing; Zhang, Rukang; Jiang, Xiangrui; Hu, Tianwen; Wang, Xinjun; Qiao, Gang; Wang, Junjian; Yang, Fengling; Luo, Xiaomin; Chen, Kaixian; Shen, Jingshan; Luo, Cheng; Jiang, Hualiang; Zheng, Mingyue; European Journal of Medicinal Chemistry; vol. 163; (2019); p. 281 – 294;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – 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 486460-21-3 as follows. Product Details of 486460-21-3

To a stirring mixture of 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[l,2,4]triazolo[4,3-a]pyrazine (5.00 g, 26.0 mmol) and sodium tungstate dihydrate (0.343 g, 1.04 mmol) in water (5 mL) at 0 C was added 30% hydrogen peroxide soln (6.1 mL) dropwise over 15 min. The reaction was warmed to rt, kept at rt for 5 min, then cooled again over an ice bath. After 20 min sodium bisulfite (lg) was added portionwise followed by CH2CI2 (300 mL), MeOH (30 mL) and NaCl to saturate the mixture. After stirring for 16h the solids were allowed to settle and the liquids were decanted away. The solids were washed with 10% MeOH/CH2Cl2. The organics were combined, dried with Na2S04, filtered and concentrated in vacuo. The residue was purified by flash chromatography (Si02, 0-10% (10% 2N NH3/MeOH)/DCM) to obtain the product as a yellow oil (5.36 g, 26%).

According to the analysis of related databases, 486460-21-3, the application of this compound in the production field has become more and more popular.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; ANDRES GIL, JOSE IGNACIO; LETAVIC, MICHAEL A; RECH, JASON C; RUDOLPH, DALE A; SOYODE-JOHNSON, AKINOLA; CHROVIAN, CHRISTA C; (158 pag.)JP2017/527588; (2017); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Adding a certain compound to certain chemical reactions, such as: 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, belongs to pyrazines 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 486460-21-3, Formula: C6H7F3N4

To a solution of the acid (VII?) (300 mg, 0.90 mmol) and triazolopiperazine (VIII) (170 mg, 0.90 mmol) in CH2Cl2 (10 mL) is added N-hydroxybenzotriazole (150 mg, 1.08 mmol), and 10 minutes later, EDC (260 mg, 1.35 mmol). The mixture, under an inert atmosphere of N2, is magnetically stirred for 4 hours until completion, then a saturated solution of sodium bicarbonate (5 mL) is added and the mixture is extracted with dichloromethane. The combined organic phases are dried and evaporated under reduced pressure. The product is purified by flash chromatography, obtaining 406 mg (86% yield) of a crystalline white solid, compound (IX?). 1H NMR (300 MHz, d6-dmso, 100 C.) delta 7.4-7.2 (m, 7H), 6.90 (bs, 1H) 4.97 & 4.90 (AB system, J=12.9 Hz, 2×1H), 4.92 (s, 2H), 4.26-4.14 (m, 3H), 3.97 (t, J=5.5 Hz, 2H), 2.92 & 2.67 (2×dd, J=14.1, 4.9 Hz, 2×1H), 2.83-2.72 (m, 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; CHEMO IBERICA S.A.; Rasparini, Marcello; Tufaro, Roberto Rocco; Minelli, Cosima; US2014/81026; (2014); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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. 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. Application In Synthesis of 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

2-(2,4-Dichlorophenyl)-3-cyano-4-methylsulfonylethyl-6-methylpyridine(Compound III, 0.53 g, 1.38 mmol), DIPEA (0.53 g, 4.14 mmol)Soluble in 10ml DMF,After heating to 60 C for 2.5 h, add 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-alpha]pyrazine (0.53 g, 2.76 mmol),The temperature was raised to 90 C and stirred for 5 h. The reaction solution was added to 20 ml of water and extracted with EA (10 ml×2).The organic phases were combined, dried over anhydrous sodium sulfate and suction filtered.Concentrated column (CH2Cl2/MeOH)A pale yellow oil was obtained in 0.47 g, yield 71%.

The synthetic route of 486460-21-3 has been constantly updated, and we look forward to future research findings.

Synthetic Route of 486460-21-3, 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 486460-21-3 as follows.

Example 22: Preparation of ((R)-3-(methoxyamino)-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (formula 16, R2=OMe) [Show Image] 6.0 g of compound of formula 15, 0.3 g 1-hydroxybenzotrizole hydrate (HOBt) and 4.7 g 3-(trifluoro-methyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine were dissolved in 40 mL of dry dichloromethane. To the clear solution 4.5 mL of N,N’-diisopropylcarbodiimide were added during stirring at 20 C. After addition, the reaction mixture was kept stirring for 2 hours at 23 C, followed by cooling the reaction mixture to 0 C for 2 hours. The precipitate was filtered-off and discarded. The filtrate was evaporated at 45 C and 5 mbar of final pressure, obtaining 12.0 g of crude product.

According to the analysis of related databases, 486460-21-3, the application of this compound in the production field has become more and more popular.

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. 486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. Quality Control of 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine

3.0 g of intermediate V (4.5 mmol) was dissolved in 25 mL of DMF,2.06 g of EDC.HCl (10.8 mmol) and1.46 g of HOBT (10.8 mmol) followed by 1.80 g of starting material X (9.0 mmol) and 1.30 mL of triethylamine (9.0 mmol)Stirred at room temperature for 15 h,Add water to extract the reaction,Ethyl acetate extraction, organic NaHCO3 aqueous solution and saturated brine,No waterNa2SO4. The solvent was evaporated under reduced pressure and the column chromatography (EtOAc / petroleum ether = 7: 3) gave the product as a white solid intermediate

The synthetic route of 486460-21-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Guizhou University; Liu Xiongli; Tian Minyi; Yao Zhen; Liu Xiongwei; Zhang Min; Zhou Ying; Feng Tingting; Yu Zhangbiao; (6 pag.)CN107129501; (2017); A;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

486460-21-3, name is 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine, belongs to pyrazines compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Recommanded Product: 486460-21-3

Example 19E (66 mg, 0.18 mmol), 3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine (prepared as described in D. Kim et al, J. Med. Chem. 2005, 48, 141-151). 41.6 mg, 0.216 mmol), and triethyl amine (62.6 mL, 0.45 mumol) were mixed in 1 mL of methylene chloride and stirred for two days. The mixture was then purified by flash chromatography (eluting with 60-70% ethyl acetate/hexane) to give the desired nitro amine.

The synthetic route of 486460-21-3 has been constantly updated, and we look forward to future research findings.