Month: June 2021

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.4928-88-5, name is Methyl 1H-1,2,4-triazole-3-carboxylate belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. COA of Formula: C4H5N3O2

To a cooled (0 oC) solution of methyl 1H-1,2,4-triazole-3-carboxylate (36 g, 283.2 mmol, 1.0 equiv) in pyridine(300mL) was added triphenylmethyl chloride (85 g, 304.9 mmol, 1.1 equiv) and the suspension was stirred for 90 min at room temperature. Then the suspension was then heated at 100 oC and refluxed for 2h. The clear solution was cooled to room temperature and concentrated under vacuum. Isopropanol (500 mL) was added to the residue and the solid was filtered and washed with 3x 300 mL H2O. The solid was dried in an oven under reduced pressure to afford 85 g of the title compound as a white solid. LCMS ES+ 243 [M+H]+ (Trityl fragment).

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

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; BRONNER, Sarah M.; CRAWFORD, James J.; CRIDLAND, Andrew; CYR, Patrick; FAUBER, Benjamin; GANCIA, Emanuela; GOBBI, Alberto; HURLEY, Christopher; KILLEN, Jonathan; LEE, Wendy; RENE, Olivier; VAN NIEL, Monique Bodil; WARD, Stuart; WINSHIP, Paul; ZBIEG, Jason; (439 pag.)WO2018/83105; (2018); 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. 4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Formula: C3H3N3O2

A mixture of 3-(6-phenylpyridin-3-yl)-5-(piperidin-4-yl)-8,9- dihydropyrazolo[l,5-a]pyrido[3,2-e]pyrimidin-6(7H)-one (70 mg, 0.17 mmoL), 1H- 1,2,4- triazole-3-carboxylic acid (20.5 mg, 0.18 mmoL), EDC (63 mg, 0.33mmoL), HOBt (44.6 mg, 0.33 mmoL) and DIEA (172.2 uL, 0.99 mmoL) in DMF (3 mL) was stirred at room temperature for 2h. Purification with prep-LC provided 5-(l-(4H-l ,2,4-triazole-3- carbonyl)piperidin-4-yl)-3~(6-phenylpyridin-3-yl)-8,9-dihydropyrazolo[l,5-a]pyrido[3s2- e]pyrimidin-6(7H)-one: LCMS tR = 3.15 Min (10 rain run, UV 254nm)- Mass calculated for, M+ 519.2, observed LC/MS m/z 519.97 (M+H).

If you are hungry for even more, make sure to check my other article about 4928-87-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; SCHERING CORPORATION; MENG, Zhaoyang; REDDY, Panduranga Adulla, P.; SIDDIQUI, M. Arshad; MANDAL, Amit, K.; LIU, Duan; ZHAO, Lianyun; MCRINER, Andrew; WO2012/27234; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 4928-88-5, 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. 4928-88-5, name is Methyl 1H-1,2,4-triazole-3-carboxylate, molecular formula is C4H5N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

A solution of [L-TRITYL-LH-[1,] 2,4] triazole-3-carboxylic acid methyl ester (4.7 g, 0.12 mol) in tetrahydrofuran was added dropwise to a suspension of lithium aluminum hydride (724 mg, 0.12 mol) in tetrahydrofuran (63 mL) cooled to [0 oC.] The reaction mixture was allowed to gradually warm to [25 oC.] The reaction was then stirred at 25 [oC] for 48 h. At this time, the reaction was cooled to [0 oC] and diluted with ethyl acetate (140 mL). The reaction mixture was then consecutively treated with water (0.925 mL), a 15percent aqueous sodium hydroxide solution (0.925 mL), and water (2.8 mL). This mixture was stirred at [0 oC] for 15 min. At this time, magnesium sulfate was added. The resulting mixture was filtered to remove the solids. The solids were washed with tetrahydrofuran and dichloromethane. The filtrate was concentrated in vacuo to afford [(L-TRITYL-LH-[1,] 2,4] triazol-3-yl) -methanol (2.2 g, 51percent) as a white solid

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 Methyl 1H-1,2,4-triazole-3-carboxylate, hurry up and to see.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; WO2003/106459; (2003); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 4928-87-4, 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. 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 2 1-(1-(1H-1,2,4-triazole-3-carbonyl)piperidin-3-yl)-3-methyl-8-(6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)-1H-imidazo[4,5-c]quinolin-2(3H)-one 20 mg (0.0455 mmol) of Compound 111, 6.2 mg (0.0546 mmol) of 1H-1,2,4-triazole-3-carboxylic acid, 9.23 mg (0.0683 mmol) of HOBt and 13.09 mg of EDCI were suspended in 2 ml of dichloromethane, added with 13.9 mg (0.137 mmol) of triethylamine, and stirred at room temperature for 4 h. TLC (DCM: MeOH = 10: 1) showed that most of the raw materials were not reacted. 9.3 mg of 1H-1,2,4-triazole-3-carboxylic acid, 26 mg of HATU and 15 mg of triethylamine were supplemented, and stirred at room temperature overnight. TLC (DCM: MeOH = 10: 1) showed that most of the raw materials were reacted completely. 10 mL of saturated sodium bicarbonate solution was added and stirred for 1 h. The organic phase was separated off, and the aqueous phase was extracted with 2 * 5 ml of dichloromethane. The organic phases were combined, dried, evaporated to dryness, and purified by preparative TLC (dichloromethane: methanol = 10: 1) to afford the target compound of Example 2 (17.8 mg), as a light yellow powder. Yield: 73%. LC-MS: 535 [M+1]+, tR = 1.463 min. 1H NMR (400 MHz, DMSO+D2O) delta 9.41 (d, J = 7.9 Hz, 1H), 9.14 (d, J = 6.0 Hz, 1H), 9.00 – 8.91 (m, 1H), 8.87 – 8.79 (m, 1H), 8.78 – 8.65 (m, 2H), 8.64 – 8.44 (m, 2H), 8.39 (s, 1H), 8.22 – 7.96 (m, 1H), 5.56 – 4.07 (m, 3H), 4.00 (d, J = 16.3 Hz, 3H), 3.60 (d, J = 13.2 Hz, 3H), 3.44 – 3.17 (m, 2H), 3.00 – 2.82 (m, 1H), 2.31 – 2.14 (m, 1H).

Future efforts will undeniably focus on the diversification of the new catalytic transformations. These may comprise an expansion of the substrate scope from aromatic and heteroaromatic compounds to other hydrocarbons. Keep reading other articles of 4928-87-4.

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

Reference of 15988-11-1, 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. 15988-11-1, name is 4-Phenyl-1,2,4-triazolidine-3,5-dione, molecular formula is C8H7N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

General procedure: General procedure: A mixture of 4-phenylurazole (1, 1 mmol), aryl aldehyde (2, 1.1 mmol) or ketone (5, 1.1 mmol), 1,3-diketone (3, 1 mmol) and FeCl3 (16.2 mg, 10 mol%) in acetonitrile (2.5 mL) was stirred in preheated oil bath at reflux for a specified time as required to complete the reaction (see Table 2 and 3). After complete conversion, as indicated by TLC, the solvent was removed in vacuo and the residue was diluted with water and extracted with ethyl acetate (2×10 mL). The combined organic layers were dried over anhydrous Na2SO4, concentrated in vacuo and purified by column chromatography on silica gel (Merck, 60-120 mesh, ethyl acetate:hexane, 4:6) to afford the pure triazolo[1,2-a]indazoletrione or spirotriazolo[1,2-a]indazoletetraonederivative.

I am very proud of our efforts over the past few months and hope to 4-Phenyl-1,2,4-triazolidine-3,5-dione help many people in the next few years.

Reference:
Article; Subba Reddy; Umadevi; Narasimhulu; Yadav; Chemistry Letters; vol. 42; 8; (2013); p. 927 – 929;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 342617-08-7, New Advances in Chemical Research in 2021.Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, 342617-08-7, name is 3-(3-Bromophenyl)-4H-1,2,4-triazole, molecular formula is C8H6BrN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

A slurry of 3-(3-bromophenyl)-1H-1,2,4-triazole (58.5 g; 261 mmol; Step 1 above), anhydrous K2CO3(43.2 g; 313 mmol), and chloromethylpivalate (45 mL; 313 mmol) in dry MeCN (250 mL) was heated to 80 C. (Note 1) for 1 hour. The mixture was cooled, solid was collected by filtration and the filtrate was concentrated in vacuo. Residue from the filtaret was combined with the filtered solid and the whole was stirred with water approximately 20 minutes. Solid was collected by filtration, washed with water (×3) and recrystallized from MeOH/water, affording the title compound as a colorless solid.

We very much hope you enjoy reading the articles and that you will join us to present your own research about 342617-08-7, Happy reading!

Reference:
Patent; SMITHKLINE BEECHAM CORP; COWAN, D. J; LARKIN, A. L.; ZHANG, CUNYU; MUSSO, D. L.; GREEN, G. M.; CADILLA, R.; SPEARING, P.K.; BISHOP, M. J.; SPEAKE, J. D.; (219 pag.)CN102516115; (2016); B;,
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. 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

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.

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 1H-1,2,3-Triazole help many people in the next few years.

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

Synthetic Route of 7170-01-6, New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 7170-01-6, name is 3-Methyl-1H-1,2,4-triazole, 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.

((2S,3S)-3-(((benzyloxy)carbonyl)amino)-1-(2,4-dimethoxybenzyl)-4-oxoazetidin-2-yl)methyl methanesulfonate (3.74 g, 8.0 mmol), 3-methyl-1H-1,2,4-triazole (2.00 g, 24.0 mmol), K2CO3 (6.64 g, 48.0 mmol) and NaI (2.88 g, 17.2 mmol) were slurried in DMF (16 mL) and heated to 70 C. with stirring. After 24 h the mixture was concentrated in vacuo. The crude residue was purified via silica gel chromatography (MeOH-DCM, 2%) to afford title compounds (1.64 g, 44% combined) as an off-white solid (unseperable mixture). LCMS: m/z=466.2 (M+1).

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 3-Methyl-1H-1,2,4-triazole, hurry up and to see.

Reference:
Patent; NOVARTIS AG; AULAKH, Virender Singh; CASAREZ, Anthony; LIN, Xiaodong; LINDVALL, Mika; MCENROE, Glenn; MOSER, Heinz Ernst; RECK, Folkert; TJANDRA, Meiliana; SIMMONS, Robert Lowell; YIFRU, Aregahegn; ZHU, Qingming; US2015/266867; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 16681-70-2, 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. 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.

lH-l,2,3-triazole-4-carboxylic acid (15.9 mg, 141 muiotaetaomicron) and HATU (53.5 mg, 141 muiotaetaomicron) were dissolved in DMF (2 mL) and stirred for 15 minutes at room temperature. (2R,^R)-4-Amino-2-azido-5-(5′-chloro-2′-fluorobiphenyl-4-yl)pentanoic acid ethyl ester (50 mg, 128 muiotaetaomicron) and DIPEA (67 mu^, 384 muiotaetaomicron) were added, and the mixture was stirred at room temperature for 15 minutes then concentrated in vacuo and the residue was dissolved in EtOH (2 mL). An aqueous solution of IN NaOH (1.3 mL, 1.3 mmol) was added, and the mixture was stirred at room temperature for 30 minutes then concentrated in vacuo and the residue was purified by reverse phase chromatography to yield Compound 1 (45 mg).

Future efforts will undeniably focus on the diversification of the new catalytic transformations. These may comprise an expansion of the substrate scope from aromatic and heteroaromatic compounds to other hydrocarbons. Keep reading other articles of 16681-70-2.

Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; FLEURY, Melissa; BEAUSOLIEL, Anne-Marie; HUGHES, Adam D.; LONG, Daniel D.; WILTON, Donna A.A.; WO2015/116786; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 7343-34-2, New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 7343-34-2, name is 3,5-Dimethyl-4H-1,2,4-triazole, 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.

Under an atmosphere of argon, (2S,4R)-N-(1-cyanocyclopropyl)-4-(4-fluorophenylsulfonyl)- 1- (1- (trifluoromethyl)cyclopropanecarbonyl)pyffolidine-2-carboxamide (example 33, step b, 0.1 g, 211 imol) was combined with N,Ndimethylacetamide (2.00 mL) to give a colorless suspension. 3,5-Dimethyl-1H-1,2,4- triazole (41.0 mg, 422 imol) and cesium carbonate (138 mg, 422 imol) were added.The reaction mixture was stirred over the weekend at ambient temperature. The crude materialwas purified by preparative HPLC (Zorbax Eclipse XDB-C18; 21,2x50mm; flow: 25 mL/min; gradient: acetonitrile / water (+0.1percent formic acid) = (95percent-5percent to 5percent-95percent) in 6 mm; collected by 254 nm detector) to yield the title compound as a colorless viscous oil (13.2 mg, 11.4 percent). mlz = 551.17 [M+H41.

This is the end of this tutorial post, and I hope it has helped your research about 7343-34-2!

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HAAP, Wolfgang; KUHN, Bernd; LUEBBERS, Thomas; PETERS, Jens-Uwe; (93 pag.)WO2017/144483; (2017); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics