Day: April 14, 2021

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 4928-87-4 as follows. name: 1,2,4-Triazole-3-carboxylic acid

To a reaction of 1/7-1, 2, 4-triazole-3 -carboxylic acid (226 mg, 2.0 mmol) and (2,3- dimethoxybenzyl)amine (0.31 mL, 2.1 mmol) in dry DMF (10 mL) was added 1- hydroxybenzotriazole monohydrate (337 mg, 2.2 mmol) and EDC (N-(3- Dimethylaminopropyl)-N’-ethylcarbodiimide) (422 mg, 2.2 mmol) followed by N- methylmorpholine (0.88 mL, 8.0 mmol via syringe). The mixture was stirred at room temperature under nitrogen and the solids were gradually dissolved. The contents were stirred at room temperature for 24 h, and then slowly diluted into ice cold water and extracted with DCM (2 x 50 mL). The DCM phase was washed with ice cold water (2 x 100 mL). The DCM phase was dried over anhydrous Na2S04, filtered and concentrated under reduced pressure and chromatographed on silica gel using EtOAc and Hexanes (9: 1) as eluents to get the desired amide 3 (104.9 mg, 20% yield) as a white solid. -NMEI (400 MHz, DMSO-de): <514.67 (br s, 1H), 8.94 (br s, 1H), 8.49 (br s, 1H), 7.03-6.99 (m, 1H), 6.99-6.94 (m, 1H), 6.85-6.82 (m, 1H), 4.48 (d, J= 6.4 Hz, 2H), 3.80 (s, 3H), 3.78 (s, 3H) ppm. MH+ = 233.2 m/z. According to the analysis of related databases, 4928-87-4, the application of this compound in the production field has become more and more popular. Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE; NATIONAL JEWISH HEALTH; WEMPE, Michael Fitzpatrick; VAZQUEZ-TORRES, Andres; DAI, Shaodong; (72 pag.)WO2020/41556; (2020); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

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. 7411-23-6, name is 3,5-Dibromo-1H-1,2,4-triazole, This compound has unique chemical properties. The synthetic route is as follows., category: Triazoles

2,2′-Bipyridine (3.12, 20 mmol), copper acetate (3.63 g, 20 mmol) and sodium carbonate (4.24 g, 40 mmol) was added to a solution of 3,5-dibromo-lH-l,2,4-triazole (4.54 g, 20 mmol) and cyclopropyl boronic acid (3.44 g, 40 mol) in DCE (150 ml). The r.m. was heated at 70 C for 16 h and was then cooled to r.t. and washed with a sat. aq. solution of ammonium chloride. The combined organic extracts were washed with brine and dried (MgS04). Filtration and concentration under reduced pressure gave a residue which was purified by flash column chromatography over silica gel (eluent:Heptane/EtOAc from 100/0 to 50/50). The product fractions were collected and concentrated in vacuo, yielding 1 g of a 70/30 mixture of intermediate 69 andintermediate 70 (21 %) which was used as such in the next reaction step.

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 7411-23-6.

Reference:
Patent; ORTHO-MCNEIL-JANSSEN PHARMACEUTICALS, INC; VAN BRANDT, Sven, Franciscus, Anna; DE CLEYN, Michel, Anna, Jozef; GIJSEN, Henricus, Jacobus, Maria; BERTHELOT, Didier, Jean-Claude; SURKYN, Michel; WO2011/86099; (2011); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 7411-23-6, 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. 7411-23-6, name is 3,5-Dibromo-1H-1,2,4-triazole belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below.

First, 43.7 g of 3,5-dibromo-1H-1,2,4-triazole is introduced into 200 mL of tetrahydrofuran (THF), the resultant mixture is agitated, and 40.4 g of 2-chloro-2,4-difluoroacetophenone is further introduced thereto. Next, 36.3g of potassium carbonate is introduced to the reaction mixture and the resultant mixture is agitated for 7 hours at room temperature. After the completion of the reaction, the reaction mixture is filtered, washed with 100 mL of tetrahydrofuran (THF), andconcentrated at room temperature. Then, 437 mL of purified water is introduced so that the crystals are slurried, followed by filtering. The filtered crystals are reslurried in 175 mL of isopropanol and filtered again. The crystals are washed with 44 mL of isopropanol and dried with hot air at 50C to obtain 63.8 g of the title compound as a white solid (yield 87%, purity 99.2%, HPLC, detected at a wavelength of 256 nm, 18C 4.6 X 250 mm, mobile phase 60% ACN, flow rate 1 mL/min). [96] 1H-NMR (200MHz, CDCl3) delta (ppm) : 8.11~8.03(1H), 7.11-6.96(2H), 5.51(2H).

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, 3,5-Dibromo-1H-1,2,4-triazole, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; DONGKOOK PHARMACEUTICAL CO., LTD.; KWON, Hyuk Chul; RHO, Man Dong; CHA, Kyung Hoi; WO2011/96697; (2011); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 288-36-8, 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. 288-36-8, name is 1H-1,2,3-Triazole, This compound has unique chemical properties. The synthetic route is as follows.

In a dry Schlenk Tube at RT under nitrogen are successively charged 2-fluoro-6-iodo-3- methyl-benzoic acid (1.786 mmol, 1 eq), Cul (0.089 mmol, 0.05 eq), 1 H-1 ,2,3-triazole (3.571 mmol, 2 eq), Cs2C03 (3.571 mmol, 2 eq) and DMF (2.5 mL). The resulting blue suspension is stirred at 80C overnight. The obtained reaction mixture is taken up in 1 M aq. HCI and extracted twice with EtOAc. The combined organic layers are dried over Na2S04, filtered and concentrated under reduced pressure. Purification is achieved by preparative HPLC (conditions D) to give the titled compound (246 mg) as a pale yellow solid. LC-MS (conditions A): tR = 0.55 min, [M + 1 ]+ = 222.19.

The chemical industry reduces the impact on the environment during synthesis 1H-1,2,3-Triazole. I believe this compound will play a more active role in future production and life.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; BOSS, Christoph; BROTSCHI, Christine; HEIDMANN, Bibia; SIFFERLEN, Thierry; WILLIAMS, Jodi T.; WO2012/85857; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

1455-77-2, name is 3,5-Diamino-1,2,4-triazole, belongs to Triazoles compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: Triazoles

A mixture of Zn(NO3)2?6H2O (0.029 g, 0.10 mmol), Hnic(0.036 g,0.10 mmol), Hdatrz (0.01 g, 0.1 mmol), H2O (2 mL), andDMF (2 mL) was placed in a small vial. The resulting mixture was stirred for 30 min at room temperature, and thenthe mixture was kept at 110C for three days. After beingslowly cooled to the room temperature, colorless block crystals of 1were isolated in 35percent yield based on Zn(II). Anal. Calcd. for C16H16N12O4Zn2(571.19): C, 33.61; N, 29.41; H,2.80percent. Found: C, 33.62; N, 29.38; H, 2.84percent.

The synthetic route of 1455-77-2 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Bu, Xianzhong; Chen, Jinquan; Hu, Mingzhen; Synthesis and Reactivity in Inorganic, Metal-Organic, and Nano-Metal Chemistry; vol. 46; 1; (2016); p. 123 – 126;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 956317-36-5, 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. 956317-36-5, name is 5-Methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below.

A mixture of 12 (1.3 g, 6.3 mmol), HATU(4.7 g, 12.6 mmol) and TEA (1.2 g, 12.6 mmol) in DCM (30 mL) was stirred at r.t. for30 min. Then 23 (1.5 g, 6.3 mmol) was added, the reaction was stirred at r.t. for 1 hr.The mixture was diluted with water and extracted with EtOAc. The organic layers was concentrated and purified by silica gel chromatography (eluting with DCM) to give 24 (1.3 g, yield: 73%). MS (ESI): m/z 424.2 [M + H]+.

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, 5-Methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Wu, Songliang; Sun, Yu; Hu, Yi; Zhang, Hongmei; Hou, Lijuan; Liu, Xing; Li, Yufeng; He, Haiying; Luo, Zhi; Chen, Yuan; Wang, Yuhe; Shi, Weihua; Shen, Liang; Cao, Changqing; Liang, Wei; Xu, Qing; Lv, Qiang; Lan, Jiong; Li, Jian; Chen, Shuhui; Bioorganic and Medicinal Chemistry Letters; vol. 27; 6; (2017); p. 1458 – 1462;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 16681-70-2, These common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-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.

[0841] lH-1,2,3-triazole-5-carboxylic acid (3.4 mg, 30f.tmol) and HATU (11.4 mg, 30 Imo’) were dissolved in DMF(0.5 mL) and stirred at room temperature. A solution of (2R,4 R )-4-amino-5 -( 5′ -chloro-2′-flu oro bipheny 1-4-yl )-2-(1-iso butyry loxy-ethoxycarbony amino )pentanoic acid benzy Iester (19 mg, 27 f.tmol) in DMF (0.5 mL) was added to thissolution, followed by DIPEA (14 f.LL, 82 f.tmol). The resultingsolution was stirred at room temperature for 90 minutes andthen concentrated in vacuo. The crude residue was purified bysilica gel chromatography (0-100% EtOAc:hexanes) to yieldCompound 1 (13 mg) as a clear oil.

The synthetic route of 16681-70-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; Fleury, Melissa; Beausoliel, Anne-Marie; Hughes, Adam D.; Long, Daniel D.; Wilton, Donna A.A.; US2015/210690; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 16681-70-2, 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. 16681-70-2 name is 1H-[1,2,3]Triazole-4-carboxylic acid, 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.

1,2,3-Triazole-4-carboxylic acid (0.0274 g, 0.242 mmol), DIPEA (169 muL, 969 mumol) and HATU (92 mg, 242 mumol) were combined in DMF (0.2 mL) and stirred for 5 minutes at room temperature. This was then combined with (2S,4R)-4-amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid oxetan-3-yl ester (89.5 mg, 242 mumol), predissolved in DMF (0.2 mL) and DIPEA (0.5 eq.). The resulting mixture was stirred for 15 minutes and the reaction was quenched with AcOH. The product was purified by preparative HPLC and lyophilized to yield the title compound (17 mg; purity 95%). MS m/z [M+H]+ calc’d for C25H28N4O5, 465.21. found 465.4.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 1H-[1,2,3]Triazole-4-carboxylic acid, and friends who are interested can also refer to it.

Reference:
Patent; THERAVANCE, INC.; US2012/213806; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 288-36-8, The chemical industry reduces the impact on the environment during synthesis 288-36-8, name is 1H-1,2,3-Triazole, I believe this compound will play a more active role in future production and life.

Step A: A solution of lH-l,2,3-triazole (1.0 g, 14.5 mmol), methyl iodide (3.1 g, 21.7 mmol) and K2CO3 (4.0 g, 28.9 mmol) in THF (15 mL) was stirred at room temperature for 3 hours. EtOAc (20 mL) and H20 (10 mL) were added, separated. The solvent was concentrated under vacuum. The crude residue was purified by silica gel chromatography eluting with 10% MeOH/DCM to afford l-methyl-lH-l,2,3-triazole (860 mg, 10.4 mmol, 71% yield) as yellow oil.

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, 1H-1,2,3-Triazole, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; GENENTECH, INC.; F. HOFFMANN-LA ROCHE AG; YUK, Inn H.; PURKEY, Hans; O’BRIEN, Thomas; WO2015/142903; (2015); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

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. 288-36-8, name is 1H-1,2,3-Triazole, This compound has unique chemical properties. The synthetic route is as follows., Safety of 1H-1,2,3-Triazole

j0294] To 3-bromo-6-methylpicolinonitrile (2.2 g, ii mmol) in DMF (28 mE) was added K2C03 (i .7 g, i2 mmol) and 2H-i,2,3-triazole (650 pL, ii mmol). The mixture was heated to iOO C. for 36 h, cooled to rt and extracted with EtOAc. The combined organics were dried (Na2504) and concentrated. Purification via silica gel chromatography (i 0- i 00% EtOAc in hexanes) gave the title compound (i g, 48%).

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 288-36-8.

Reference:
Patent; Janssen Pharmaceutica NV; COATE, Heather R.; DVORAK, Curt A.; FITZGERALD, Anne E.; LEBOLD, Terry P.; PREVILLE, Cathy; SHIREMAN, Brock T.; (473 pag.)US2016/46640; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics