Category: Triazoles

Electric Literature of 7170-01-6, New Advances in Chemical Research in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 7170-01-6, name is 3-Methyl-1H-1,2,4-triazole, molecular formula is C3H5N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

3-Methyl-iH-i,2,4-triazole (375 mg, 4.51 mmol) was placed in a flask with dry DMF (5 mL).Sodium hydride (195 mg, 4.89 mmol) was added and the RM was stirred at room temperature for 15 minutes. tert-Butyl 4-((methylsulfonyl)oxy) pi peridi ne-i -carboxylate (Intermediate C, step 1) (i.OOg, 3.S8mmol) was then added and the RM was stirred at 10000 for 4 hours. The resulting mixture was partitioned between EtOAc and water. The organic phase was washed with water and brine, dried over Mg504, filtered and the solvent wasremoved in vacuo. The product was purified by chromatography on silica eluting with isohexane/( EtOAc:MeOH – 10:1) to afford:Product Step 1 a: tert- Butyl 4-(3-methyl- 1 H- 1,2 ,4-triazol- 1 -yl)piperidine- 1 -carboxylate;1H NMR (400 MHz, DMSO-d6) O 8.40 (iH, 5), 4.48 (iH, m), 4.01 (2H, m), 2.90 (2H, m), 2.22(3H, 5), 1.99 (2H, m), 1.72 (2H, m), 1.40 (9H, 5).Product Step 1 b: tert- Butyl 4-(5-methyl- 1 H- 1,2 ,4-triazol- 1 -yl)piperidine- 1 -carboxylate;1H NMR (400 MHz, DMSO-d6) O 7.79 (iH, 5), 4.45 (iH, m), 4.02 (2H, m), 2.90 (2H, m), 2.41 (3H, 5), 1.82 (2H, m), 1.75 (2H, m), 1.41 (9H, 5).

This is the end of this tutorial post, and I hope it has helped your research about 7170-01-6!

Reference:
Patent; NOVARTIS AG; BEATTIE, David; BAETTIG, Urs; LEGRAND, Darren Mark; LISTER, Andrew Stuart; MCKENNA, Jeffrey; PEARCE, David William; SANDHAM, David Andrew; STEWARD, Oliver Ross; THOMSON, Christopher; WO2015/8230; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 41253-21-8, New Advances in Chemical Research in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 41253-21-8, name is Sodium 1,2,4-triazol-1-ide, molecular formula is C2H2N3Na, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

EXAMPLE 30 Preparation of bis(4-Fluorophenyl)methyl(1H,-1,2,4-triazol-1-ylmethyl)silane and its hydrochloride salt A mixture of 4.2 g (0.015 mol) of (chloromethyl)bis(4-fluorophenyl)methylsilane and 1.4 g (0.015 mol) of 1,2,4-triazole sodium salt in 8 ml of dimethylformamide was stirred at 80 for 2 hours. The resulting slurry was cooled, diluted with water, and washed with ether. The ether extracts were washed with several portion of water and once with brine, dried over magnesium sulfate, and evaporated to leave 4.0 g of a pale yellow oil. Impurities were removed by Kugelrohr distillation at 120-125 (0.05 mm), leaving behind 2.3 g (49%) of the title compound as a yellow oil: nD21 1.5538; ir (neat) 3065, 3030, 2960, 2925, 1590, 1500, 1270, 1235, 1165, 1110, 1010, 830, 790 cm-1; nmr (CDCl3): 0.7 (3H, s), 4.2 (2H, s), 7.1 (4H, t, J=9), 7.5 (4H, d of d, J=6 and 9), 7.8 (1H, s) and 7.9 (1H, s). A sample prepared similarly was crystallized from hexane at -20 C. to give colorless solid, m.p. 52-53. The hydrochloride salt of the title compound was prepared as follows. A solution of 5.0 g (0.016 mol) of [bis(4-fluorophenyl)]methyl(1H-1,2,4-triazol-1-ylmethyl)silane in 100 ml of toluene was stirred while HCl gas was passed over the solution surface until no further precipitate formed. The colorless solid was collected by filtration, washed with toluene and petroluem ether, and air-dried to give 5.1 g (91%) of the hydrochloride salt, m.p. 195-197. Recrystallization from 100 ml of hot ethanol gave 3.5 g of colorless crystals, m.p. 201-203. Acid salts of the other triazoles of this invention can be prepared similarly. By applying the procedures of Examples 24 and 26-30 to appropriate chloromethylsilanes, the compounds of Table VI can be prepared.

I am very proud of our efforts over the past few months and hope to Sodium 1,2,4-triazol-1-ide help many people in the next few years.

Reference:
Patent; E. I. Du Pont de Nemours and Company; US4510136; (1985); A;,
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.7343-33-1, name is 5-Bromo-1H-1,2,4-triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. category: Triazoles

To a suspension of 3-bromo-1H-i,2,4-triazole (lOg, 67.6mM) and phenylboronic acid (16.5g, 135.2mM) in 500 mL of DCM, was added the following: pyridine; (i0.9mL, i0.7g, 135.2mM), copper (II) acetate; (1 8.4g, 101.5mM) and powdered 4A molecular sieves (45g). The resulting blue colored suspension was stined at room temperature for 10 days open to the air. Additional DCM (500mL) was added to the reaction and the mixture filtered through a pad of diatomaceous earth, washing the cake with DCM, 10percent MeOH/DCM, and finally DCM. The filtrates were collected and concentrated under reduced pressure to provide a viscous residue, which was partitioned between ethyl acetate and iN HC1. The organic phase was washed with water (2x), brine (ix) then dried over anhydrous sodium sulphate. Suction filtered the organic layer to remove particulates and evaporated under reduced pressure to give the crude product which was purified on CombiFlash (240g column) 5i02 eluting with 25percent ethyl acetate /heptanes. Combined clean fractions and reduced the volume of the fractions under reduced pressure until crystals formed. Isolated crystals via suction filtration, washed with additional heptanes and air dried to yield 3-bromo-i-phenyl-1H-i,2,4-triazole as a white crystalline solid (5.ig, 34percent yield). ?H NMR (400 MHz, DMSO-d6) oe 9.32(s, 1H), 7.92 – 7.79 (m, 2H), 7.58 (dd, J=ii.3, 4.5Hz, 2H), 7.51-7.41 (m, 1H) ppm. ESI-MS m/z calc. 222.9745, found 224.0 (M+i)+; Retention time: 0.75 minutes.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 5-Bromo-1H-1,2,4-triazole ,and how the biochemistry of the body works.

Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; DAVIES, Robert, J.; CAO, Jingrong; COCKERILL, Meghan, Elise; COLLIER, Philip, Noel; DENINNO, Michael, Paul; DOYLE, Elisabeth; FRANTZ, James, Daniel; GAO, Huai; GOLDMAN, Brian, Anthony; GREY, Ronald, Lee; GRILLOT, Anne-laure; GU, Wenxin; HENDERSON, James, A.; IRARRAZAVAL, Raul Eduardo, Krauss; KOLPAK, Adrianne, Lynn; LIAO, Yusheng; MAGAVI, Sanjay Shivayogi; MALTAIS, Francois; MESSERSMITH, David; PIERCE, Albert, Charles; PEROLA, Emanuele; RYU, Elizabeth Jin-Sun; SYKEN, Joshua; WANG, Jian; (706 pag.)WO2016/197009; (2016); 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. Product Details of 288-36-8

Intermediate E: 2-(2H-l,2,3-triazol-2-yl)benzoic acid Int E Step 1 : 2-(2H-l,2,3-triazol-2-yl)benzoic acid (Int E) To a solution of 2-iodobenzoic acid (3.0 g, 12.1 mmol) in DMF was added 1,2,3-triazole (1.5 g, 21.7 mmol), Cs2C03 (7.1 g, 21.7 mmol), Cul (114 mg, 0.6 mmol), and trans-N,N’-dimethylcyclohexane- 1,2-diamine (310 mg, 2.2 mmol). After heating at 120 C for 10 min in a microwave reactor, the mixture was cooled to room temperature, diluted with EtOAc, and filtered through Celite. The filtrate was concentrated in vacuo and the crude residue was purified by silica gel chromatography (MeOH in DCM with 0.1% AcOH) to give Int E as the faster eluting isomer. 1H NMR (DMSO-d6, 500MHz) delta 13.05 (brs, 1 H), 8.12 (s, 2H), 7.81-7.52 (m, 4H).

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.; KUDUK, Scott, D.; REGER, Thomas, S.; ROECKER, Anthony, J.; WO2015/95111; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Research speed reading in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 41253-21-8, name is Sodium 1,2,4-triazol-1-ide belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. SDS of cas: 41253-21-8

(ii) Preparation of crude anastrozole; Into a 1 L, three-necked RB flask was charged 60g of sodium triazole monohydrate (prepared by reaction of molar quantities of 1,2,4-IH-triazole and sodium hydroxide in isopropanol at reflux temperature and isolated by filtering of the reaction mass at room temperature) and 200ml of dry DMF under nitrogen atmosphere. The reaction mass was cooled to 20 C. A solution of the above bromo compound of formula-V (140g) in toluene (200ml) was added to the reaction mass over a period of 2hr. The reaction mass was maintained at this temperature until the completion of reaction. The reaction mass was transferred into 3L flask containing 1.5L of water and stirred for 30min. Reaction mass was extracted with toluene (2 x 300ml and 1 x 100ml). Toluene layers were combined and washed with water (2 x 200ml). Toluene layer was treated with activated carbon (5g) and filtered. Toluene was distilled of from the filtrate under vaccum to get 130g of crude anastrozole.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 41253-21-8, and we look forward to future research findings.

Reference:
Patent; NATCO PHARMA LIMITED; PULLA REDDY, Muddasani; VENKAIAH CHOWDARY, Nannapaneni; WO2005/105762; (2005); 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. 7343-33-1, name is 5-Bromo-1H-1,2,4-triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Application In Synthesis of 5-Bromo-1H-1,2,4-triazole

To a suspension of 3-bromo-1H-1,2,4-triazole (5.0 g, 34 mmol) and cesiumcarbonate (11 g, 34 mmol) in acetonitrile (50 mL) was added 1,1,1-trifluoro-4-iodobutane (6.8 mL, 34 mmol). The solution was stirred at room temperature for 72 hours. The solution was poured into water (50 mL) and extracted with diethyl ether (2 x 100 mL). The combined organic layers were concentrated. Purification by flash column chromatography using 0-20percent ethyl acetate/hexanes as eluent, provided the titlecompound as a 70:30 mixture of isomers (3.2 g, 37percent). The mixture was used in the next step without further purification; Prepared using 4,4,5,5,5-pentafluoropentyl methanesulfonate and isolated as a light-brown liquid (3.5 g, 49percent): 1H NMR (400 MHz, CDCI3) O 7.90 (s, 1H), 4.32 – 4.30 (m, 2H), 2.27 – 2.00 (m, 4H); ESIMS m/z 308 ([M+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 5-Bromo-1H-1,2,4-triazole help many people in the next few years.

Reference:
Patent; DOW AGROSCIENCES LLC; GIAMPIETRO, Natalie C.; CROUSE, Gary D.; SPARKS, Thomas C.; (131 pag.)WO2017/40060; (2017); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

New discoveries in chemical research and development 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. 23579-79-5, name is 3,5-Dibromo-1-methyl-1H-1,2,4-triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. category: Triazoles

Bis(triphenylphosphine)palladium(II) chloride (0.087 g, 0.12 mmol) was added to a stirred mixture of tert-butyl N-tert-butoxycarbonyl-N-[3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-5-trimethylstannyl-2-pyridyl]carbamate 5a (3 g, 4.13 mmol), 3,5-dibromo-1-methyl-1,2,4-triazole 27 (1 g, 4.15 mmol) and lithium chloride (0.528 g, 12.4 mmol) dissolved in DME (8 mL) under argon. The resulting mixture was heated at 140 C for 30 min in a microwave apparatus. More bis(triphenylphosphine)palladium(II) chloride (0.087 g, 0.12 mmol) was added and the mixture was heated at 130 C for 30 min in the microwave. The mixture was evaporated under reduced pressure, adsorbed on silica gel and purified by flash chromatography on silica gel eluting with 5 to 50% ethyl acetate in dichloromethane to afford tert-butyl N-[5-(5-bromo-2-methyl-1,2,4-triazol-3-yl)-3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-2-pyridyl]-N-tert-butoxycarbonyl-carbamate (1.4 g, 58%) as a solid. Bis(triphenylphosphine)palladium(II) chloride (170 mg, 0.24 mmol) was added to a stirred mixture of tert-butyl N-[5-(5-bromo-2-methyl-1,2,4-triazol-3-yl)-3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-2-pyridyl]-N-tert-butoxycarbonyl-carbamate (1.40 g, 2.42 mmol), tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate 28 (748 mg, 2.42 mmol) and cesium fluoride (1.10 g, 7.26 mmol) in methanol (4 mL) under argon atmosphere. The resulting mixture was heated at 140 C for 40 min in a microwave apparatus. More bis(triphenylphosphine)palladium(II) chloride (1.02 g, 1.45 mmol) was added and the mixture was degassed and heated at 140 C for 30 min in the microwave. After cooling, the mixture was adsorbed on silica gel with methanol / ammonia and was purified by flash chromatography on silica gel eluting with 1 to 4% methanolic ammonia (7 N) in dichloromethane. The solvent was evaporated to dryness to afford tert-butyl 4-(5-(6-(tert-butoxycarbonylamino)-5-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyridin-3-yl)-1-methyl-1,2,4-triazol-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate (956 mg, 68%) as a yellow solid. A slurry of palladium (175 mg, 1.65 mmol) and tert-butyl 4-(5-(6-(tert-butoxycarbonylamino)-5-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyridin-3-yl)-1-methyl-1,2,4-triazol-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate (956 mg, 1.65 mmol) and ammonium formate (1.04 g, 16.5 mmol) dissolved in DMF (30 mL) was heated at 70 C for 2 h. More palladium (175 mg, 1.65 mmol) was added. The mixture was heated one more hour. The resulting slurry was filtered and the filtrate was concentrated to dryness. Water (50 mL) was added. The mixture was stirred for 1 h, filtered and dried under reduced pressure to afford crude tert-butyl 4-(5-(6-(tert-butoxycarbonylamino)-5-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyridin-3-yl)-1-methyl-1,2,4-triazol-3-yl)piperidine-1-carboxylate (562 mg, 59%) as a yellow solid. Trifluoroacetic acid (1.5 mL) was added to a stirred suspension of tert-butyl 4-(5-(6-(tert-butoxycarbonylamino)-5-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyridin-3-yl)-1-methyl-1,2,4-triazol-3-yl)piperidine-1-carboxylate (562 mg, 0.96 mmol) in dichloromethane (2 mL). The resulting solution was stirred at 25 C for 1 h. The solvents were evaporated. Traces of TFA were removed by azeotroping with toluene. The crude product was dissolved in methanolic solution of ammonia, adsorbed on silica gel, and purified by flash chromatography on silica gel eluting with 2 to 8% methanolic ammonia (7 N) in dichloromethane. The solvent was evaporated to dryness to afford 3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-5-(1-methyl-3-(piperidin-4-yl)-1,2,4-triazol-5-yl)pyridin-2-amine (332 mg, 90%) as a beige solid. Acetyl chloride (0.022 mL, 0.31 mmol) was added over a period of 15 min to a stirred solution of 3-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-5-(1-methyl-3-(piperidin-4-yl)-1,2,4-triazol-5-yl)pyridin-2-amine (100 mg, 0.26 mmol) and triethylamine (0.073 mL, 0.52 mmol) dissolved in dichloromethane (3 mL) at 0 C. The resulting solution was stirred at 0C for 1 hour. The mixture was adsorbed on silica gel with a 7 N methanolic solution of ammonia. The crude product was purified by flash chromatography on silica gel eluting with 2 to 4% methanolic ammonia (7 N) in dichloromethane. The solvent was evaporated to dryness to afford 1-[4-[5-[6-amino-5-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-3-pyridyl]-1-methyl-1,2,4-triazol-3-yl]-1-piperidyl]ethanone 5 (80 mg, 72%) as a yellow foam.

If you are hungry for even more, make sure to check my other article about 23579-79-5, the application of this compound in the production field has become more and more popular.

Reference:
Article; Barlaam, Bernard; Cosulich, Sabina; Delouvrie, Benedicte; Ellston, Rebecca; Fitzek, Martina; Germain, Herve; Green, Stephen; Hancox, Urs; Harris, Craig S.; Hudson, Kevin; Lambert-Van Der Brempt, Christine; Lebraud, Honorine; Magnien, Francoise; Lamorlette, Maryannick; Le Griffon, Antoine; Morgentin, Remy; Ouvry, Gilles; Page, Ken; Pasquet, Georges; Polanska, Urszula; Ruston, Linette; Saleh, Twana; Vautier, Michel; Ward, Lara; Bioorganic and Medicinal Chemistry Letters; vol. 25; 22; (2015); p. 5155 – 5162;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 4928-87-4, New Advances in Chemical Research in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 4928-87-4, name is 1,2,4-Triazole-3-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.

Example 8 1-(1-(1H-1,2,4-triazole-3-carbonyl)pyrrolidin-3-yl)-3-methyl-8-(6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)-1H-imidazo[4,5-c]quinolin-2(3H)-one In an ice-water bath, 48.8 mg (0.43 mmol) of 1,2,4-triazole-3-carboxylic acid and 200.76 mg (0.528 mmol) of 2-(7-azabenzotriazole)-N,N,N’,N’-tetramethyluronium hexafluorophosphate were dissolved in 5 mL of dichloromethane, added with 97 mg (0.96 mmol) of triethylamine and stirred at 0 C for 30 minutes, then added with 100 mg (0.24 mmol) of Intermediate 145 and stirred at room temperature overnight. The reaction was monitored by TLC. After the reaction was completed, 10 mL of saturated sodium bicarbonate aqueous solution was added, stirred for 20 minutes, and separated into layers. The aqueous phase was extracted with dichloromethane, and the organic phases were combined, dried, and rotary evaporated to dryness to afford a crude product. The crude product was purified with preparative silica gel plate (dichloromethane/methanol = 10/1, V/V) to afford the target compound of Example 8 (40 mg), as a white solid. Yield: 32%.

I am very proud of our efforts over the past few months and hope to 1,2,4-Triazole-3-carboxylic acid help many people in the next few years.

Reference:
Patent; Beijing Forelandpharma Co. Ltd.; ZHANG, Xingmin; JI, Qi; WANG, Lei; GAO, Congmin; WANG, Ensi; DU, Zhenjian; GONG, Longlong; CHEN, Bo; (137 pag.)EP3072893; (2016); 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. 3179-31-5, name is 1H-1,2,4-Triazole-3-thiol belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Product Details of 3179-31-5

To a solution of 1-(benzenesulfonyloxyoctyl)-cyclopropene (480 mg, 1.55 mmol) in about 2 ml N,N-dimethylformamide was added potassium t-butoxide (19.8% in tetrahydrofuran, 734 mg, 1.55 mmol) and 1H-1,2,4-triazole-3-thiol (172 mg, 1.71 mmol.) After stirring at room temperature for about 2 hours, sodium iodide (87.7 mg, 0.775 mmol) was added. After the reaction was heated to about 50 C. for about 2 hours, water and ethyl acetate were added then the phases were separated. The isolated organic layer was washed twice with water, dried over magnesium sulfate and concentrated in vacuo. This residue was purified by column chromatography on silica gel using hexanes/ethyl acetate to give 30 mg of 70% pure 1-(1H-1,2,4-triazol-2-ylthiooctyl)-cyclopropene as an oil.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 1H-1,2,4-Triazole-3-thiol ,and how the biochemistry of the body works.

Reference:
Patent; Jacobson, Richard Martin; Kelly, Martha Jean; Wehmeyer, Fiona Linette; Evans, Karen Anderson; US2005/65033; (2005); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 16681-70-2, New Advances in Chemical Research 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. 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.

[0804] lH-1,2,3-triazole-5-carboxylic acid (3.4 mg, 30f.tmol) was combined with HATU (11 mg, 30 f.tmol) in DMF(0.3 mL) and stirred at room temperature for 10 minutes;DIPEA (1 eq.) was added and the mixture was stirred for 1minute. Compound 2 (1 0 mg, 30 f.tmol) was dissolved in DMF(0.5 mL) and DIPEA (5.2 f.LL, 30 fllllOI) was added, followedby addition of the activated acid solution. The mixture wasstirred at room temperature for 30 minutes, after which timeLCMS indicated desired product formation. Half of the crudeproduct was purified using reverse phase chromatography toyield Compound a (3.5 mg) as a TFA salt. MS m/z [M+Htcalc’d for C26H28CIF2N50 3 , 532.19; found 532. Half of thecrude product was carried to the next step without purification.

The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules.Read on for other articles about 1H-[1,2,3]Triazole-4-carboxylic acid, hurry up and to see.

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