Category: Triazoles

Electric Literature of 1001401-62-2, New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic 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.

A solution of (3R, 6R)-6-methylpiperidin-3-ol (5.31 g, 46.1 mmol), 2-(2H-l,2,3- triazol-2-yl)benzoic acid (10.5 g, 55.3 mmol), EDC (17.7 g, 92.0 mmol), l-hydroxy-7- azabenzotriazole (12.6 g, 92.0 mmol), and triethylamine (19.3 mL, 138 mmol) in DMF (300 mL) was stirred at 50 C overnight, then diluted with saturated aqueous sodium bicarbonate and extracted 3x with ethyl acetate. The organics were washed with brine, dried over magnesium sulfate, filtered, and concentrated. The crude material was purified by silica gel gradient chromatography (0-100% ethyl acetate in hexanes), providing the titled compound as a pale yellow solid. LRMS m/z (Mu+Eta) 287.3 found, 287.1 required.

I am very proud of our efforts over the past few months and hope to 2-(2H-1,2,3-Triazol-2-yl)benzoic acid help many people in the next few years.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; SKUDLAREK, Jason, W.; WO2014/137883; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 16681-70-2, New Advances in Chemical Research in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

To a stirred solution of 11-3 (0.2g, 0.36mMol), HOBT (0.05g, 0.4mMol), and IH-1, 2,3- triazole-4-carboxylic acid (0.05g, 0.4mMol) in anhydrous DMF (2mL) was added DIEA (0.18mL, 1. ImMoI) followed by EDC (0.08g, 0.4mMol). The solution was heated in the microwave reactor for 30 minutes at 800C. Solution was then treated with 0.5mL of acetic acid and was heated to 800C in the microwave reactor for lOmin. Upon cooling to room temperature, the solution was passed through a EPO syringe filter and purified on a C18 reverse phase HPLC to give 11-4 as a solid. Mass (M+l) calculated: 632.2742 observed: 632.274

We very much hope you enjoy reading the articles and that you will join us to present your own research about 16681-70-2, Happy reading!

Reference:
Patent; MERCK & CO., INC.; WO2006/135627; (2006); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 288-36-8, New Advances in Chemical Research in 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 288-36-8, name is 1H-1,2,3-Triazole, molecular formula is C2H3N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

Intermediate 14f (0556) 4,5-Dibromo-lH-triazole (0557) Br2 (930 g, 5.82 mol) was added dropwise to a stirred solution of lH-triazole (300.00 g, 4.34 mol, 252.10 mL) in H20 (2 L) at 40 to 45 °C. The resulting solution was stirred for a further 1 hour. The precipitate was filtered off and further Br2 (617.28 g, 3.86 mol) was added to the filtrate, then it was kept at 25 °C for 16 hours. A second precipitate was filtered off. The combined filtered off solids were washed with water (1 L x 3), dried under vacuum and re-crystallized from MeOH (-400 mL) to give 4,5-dibromo-lH-triazole (Intermediate 14f; 890 g, 90.39percent yield) as an off-white solid, m/z (ES+) [M+H]+ (0558) 226/228/230.

The result showed that such a combination of chemo- and biocatalysis improved the catalytic yield more than two times compared with that of sole metal catalysis.I hope my blog about 1H-1,2,3-Triazole is helpful to your research.

Reference:
Patent; ASTRAZENECA AB; WARD, Richard, Andrew; JONES, Clifford, David; FERON, James, Lyman; (80 pag.)WO2017/80980; (2017); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

New discoveries in chemical research and development in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 3641-08-5, name is 2H-1,2,4-Triazole-3-carboxamide belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. 3641-08-5

General procedure: Ribavirin biosynthesis was assayed using 5 × 109 colony-forming units (CFU) in 1 mL sodium phosphate buffer (30 mM, pH7.0) containing equimolar concentrations of uridine (Urd) and TCA(2.5 mM). Reactions were performed at 60C and 200 rpm in aperiod of 16 h.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 2H-1,2,4-Triazole-3-carboxamide help many people in the next few years.

Reference:
Article; De Benedetti, Eliana C.; Rivero, Cintia W.; Trelles, Jorge A.; Journal of Molecular Catalysis B: Enzymatic; vol. 121; (2015); p. 90 – 95;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

New discoveries in chemical research and development in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 184177-83-1, name is 1-((2S,3S)-2-(Benzyloxy)pentan-3-yl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. 184177-83-1

10 g of compound of formula A and 76 mL DMSO were added into a reaction flask at room temperature, and stirred until clarification. An alkaline solution previously prepared from 1.4 g sodium hydroxide and 6 g water was further added thereto. The mixture was stirred for 1 h. Then, 10 g of compound of formula IX was added thereto. The mixture was warmed up to 38 C. and reacted for 16 h. After the reaction was completed, the mixture was warmed up to 45 C. 6 mL water was added thereto. The mixture was stirred for 30-60 min. 154 mL water was further added thereto. The mixture was stirred for 1 h, and filtered under suction. The resultant solid was drip washed with 4×50 mL purified water to obtain a wet product. (0249) The wet product and 60 mL of 90% aqueous ethanol solution were added to a reaction flask, warmed up to 65 C., and stirred. After clarification, 1.5 g active carbon was added thereto. The mixture was stirred for 15 min, filter-pressed while hot, and washed with 15 mL of 90% aqueous ethanol solution. Then, the filtrate was warmed up to 65 C., stirred, cooled to 40-45 C. after clarification, crystallized while keeping the temperature for 1 h, further cooled to 0-5 C., crystallized while keeping the temperature for 1 h, and filtered under suction. The resultant solid was first drip washed with 5 mL of 50% aqueous ethanol solution, and then drip washed with 4×50 mL purified water. The solid was collected, placed in a ventilated oven at 50-55 C. and dried for 16 h to obtain 13.2 g of product.

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Reference:
Patent; Zhejiang Ausun Pharmaceutical Co., Ltd.; Zheng, Zhiguo; (23 pag.)US2019/71408; (2019); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

New discoveries in chemical research and development in 2021. As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world.1001401-62-2, name is 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. Recommanded Product: 1001401-62-2

Step iii) ir 3s-N-{4-[(6-FIuoro-l,3-benzot azol-2-yl)ammo]oxolaii-3-yI}-2-(2H-l,2,3- triazoI-2-y)beiizamide A solution of tran5-3-N-(6-fluoro-l,3-benzothiazol-2-yl)oxolane-3,4-diarriinehydrochloride (106 mg, 0.366 mmol), 2-(2H-l ,2,3-triazol-2-yl)benzoic acid (CAS number 1001401-62-2; 83 mg, 0.439 mmol), EDC (105 mg, 0.549 mmol), aza-HOBt (85 mg, 0.549 mmol ) and triethylamime (0.153 ml, 1 .097 mmol) in DCM (2 ml) was stirred at room temperature for 18 hours. The reaction mixture was diluted with DCM (20 ml) and washed with HC1 (aq., IM, 20 ml) and saturated sodium bicarbonate solution (20 ml). The organics were filtered through a hydrophobic frit and solvent evaporated in vacuo. This was then purified by reverse phase preparative HPLC (acetonitrile / water with 0.1% ammonia) to afford the title compound.1H NMR (400 MHz, CD2C12-d2) : delta ppm 3.58 – 3.95 (m, 2 H), 4.13 – 4.32 (m, 2 H), 4.32 – 4.51 (m, 2 H), 6.77 (br. s., 1 H), 6.96 – 7.11 (m, 1 H), 7.25 – 7.41 (m, 2 H), 7.43 – 7.53 (m, 1 H), 7.56 – 7.65 (m, 2 H), 7.76 (s, 2 H), 7.81 – 7.87 (m, 1 H)MS ES+: 425

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 2-(2H-1,2,3-Triazol-2-yl)benzoic acid ,and how the biochemistry of the body works.

Reference:
Patent; TAKEDA CAMBRIDGE LIMITED; TAKEDA PHARMACEUTICAL COMPANY LIMITED; FIELDHOUSE, Charlotte; GLEN, Angela; ROBINSON, John Stephen; FUJIMOTO, Tatsuhiko; WO2015/55994; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Research speed reading in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 288-36-8, name is 1H-1,2,3-Triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. 288-36-8

To a mixture of the product from step 2 (7.9 g, 38 mmol), cesium carbonate (24.8 g,76 mmol) and Cul (2.88 g, 7.6 mmol) in DMF (200 mL) were added 2H-[1,2,3]triazole (5.24 g,76 mmol) and N,N’-dimethyl-cyclohexane-l12-diamine (0.9 g, 6.5 mmol) and the mixture was heated to 110C overnight. The cooled reaction mixture was adjusted to ~pH 12 with 1M sodium hydroxide and extracted with EtOAc (50 mL x 3). The aqueous layer was adjusted to ~pH 4 with 1M HCl and extracted with EtOAc (50 mLx4). The extracts was dried over Na2SO4, filtered, the filtrate concentrated in vacuo and the residue purified by chromatography on silica (petroleum ether : EtOAc =10:1) to provide the title compound. LRMS m/z (M+H) 196.0 found, 196.0 required.

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 288-36-8

Reference:
Patent; MERCK SHARP & DOHME CORP.; LIVERTON, Nigel; BESHORE, Douglas C.; KUDUK, Scott D.; LUO, Yunfu; MENG, Na; YU, Tingting; WO2015/18027; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 143426-50-0, New Advances in Chemical Research in 2021.In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 143426-50-0, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, molecular formula is C9H9N3O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

General procedure: To a 25-mL Schlenk tube equipped with a magnetic stirrer, PdCl2(CH3CN)2 (0.05mol, 5mol%), Bi(OTf)3 (0.05mol, 5mol%), K2CO3 (1mmol) were added. Substrates 1 (1mmol) and MeOH (2mL) were added subsequently. The reaction tube was vacuumed and backfilled with oxygen (3 times). Then the reaction mixture was stirred at 60C for 3h in the presence of an oxygen balloon. The progress of the reaction was monitored by TLC. After completion, the reaction mixture was diluted with water and extracted with ethyl acetate. The organic layer was dried over anhydrous magnesium sulfate. Subsequently, the combined organic layer was concentrated under reduced pressure and the crude product was purified by column chromatography with hexane/ethyl acetate to afford the corresponding products 2.

We very much hope you enjoy reading the articles and that you will join us to present your own research about 143426-50-0, Happy reading!

Reference:
Article; Hu, Yongke; Li, Bindong; Tetrahedron; vol. 73; 52; (2017); p. 7301 – 7307;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Research speed reading in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 16681-70-2

F. (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 1-cyclohexyloxycarbonyloxy-ethyl ester (R7=-CH(CH3)OCOO-cyclohexyl) (2S,4S)-5-Biphenyl-4-yl-4-t-butoxycarbonylamino-2-hydroxymethyl-pentanoic acid (50 mg, 120 mumol, 1.0 eq.), DMA (1 mL), DIPEA (0.13 mL, 0.75 mmol) and 1-chloroethyl cyclohexyl carbonate (52 mg, 250 mumol, 2.0 eq.) were combined. The reaction vessel was capped and microwaved at 80 C. for 2 hours. The mixture was dried under vacuum, dissolved in MeCN (2 mL), and combined with 4 M of HCl in dioxane (500 muL). The resulting mixture was stirred at room temperature for 30 minutes. The precipitate was filtered and discarded, and the filtrate containing the intermediate was concentrated down and submitted to next step. 1,2,3-triazole-4-carboxylic acid (14 mg, 120 mumol, 0.5 eq.) and HATU (48 mg, 120 mumol, 1.0 eq) were dissolved in DMF (1 mL) and the resulting solution was stirred for 5 minutes, followed by the addition of DIPEA (44 muL) and the intermediate from last step. The mixture was stirred for 5 minutes. The reaction was quenched with water and the product dried under vacuum. The product was then purified by preparative HPLC to yield the title compound (4.8 mg, 95% purity. MS m/z [M+H]+ calc’d for C30H36N4O7, 565.26. found 565.4.

The catalyzed pathway has a lower Ea, but the net change in energy that results from the reaction is not affected by the presence of a catalyst. In my other articles, you can also check out more blogs about 16681-70-2

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

New discoveries in chemical research and development in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 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. Computed Properties of C2HBr2N3

To a sol. of 3,5-dibromo-lH-l,2,4-triazole (60 g, 264.48 mmol) in CH3CN (600 mL) were added 2-(2-bromoethoxy)tetrahydro-2H-pyran (48.01 mL, 317.38 mmol) and DIPEA (48.08 mL, 290.93 mmol). The r.m. was stirred at 90 C for 3 h. The mixture was then diluted with EtOAc and washed with a sat. aq. NaHC03 sol. and brine. The separated o.l. was dried (MgS04), filtered and the solvent evaporated in vacuo. The crude product was purified by flash column chromatography (silica; eluent: DCM/(7 N NH3 in MeOH) from 100/0 to 97/3). The product fractions were collected and the solvent evaporated in vacuo. Yield: 72 g of intermediate 45 (77% yield).

If you are hungry for even more, make sure to check my other article about 7411-23-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; JANSSEN PHARMACEUTICALS, INC.; MINNE, Garrett, Berlond; BISCHOFF, Francois Paul; GIJSEN, Henricus, Jacobus, Maria; VELTER, Adriana, Ingrid; PIETERS, Serge, Maria, Aloysius; BERTHELOT, Didier, Jean-Claude; WO2013/10904; (2013); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics