Day: September 27, 2021

Electric Literature of 74205-82-6, New Advances in Chemical Research in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 74205-82-6, name is (1H-1,2,4-Triazol-1-yl)methanol, molecular formula is C3H5N3O, 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 solution of indolines 6 (1.0 mmol) dissolved in acid (1.0 ml) in an icebath was added (1H-1,2,4-triazol-1-yl)methanol 5 (ammount as given in Table 1). Themixture was then stirred under the temperature and time given in Table 1. After completion of the reaction (TLC), the reaction mixture was poured intoice water, and 20% NaOH solution was added slowly to adjust the pH to 9. The product was extracted with dichloromethane. After removal of the solvent, theresidue was chromatographed over silica gel using dichloromethane-methanol togive 7 (yield as given in Table 1). The analytical and spectroscopic data for 7b and 7c are given below

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 74205-82-6.

Reference:
Article; He, Yi; Li, Xiaolong; Li, Jue; Li, Xiaocen; Guo, Li; Hai, Li; Wu, Yong; Tetrahedron Letters; vol. 55; 29; (2014); p. 3938 – 3941;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 27808-16-8, 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. 27808-16-8, name is 4-Methyl-1H-1,2,3-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.

4-Methyl-1 H-1 ,2,3-triazole (0.1 1 mL, 1 .85mmol) was added to a solution of 3-bromo-6- methylpyridine-2-carboxylic acid (200. mg, 0.930mmol) in 1 ,4-Dioxane (1 mL)/ Water (0.1 ml_), followed by Cul (8.86mg, 0.050mmol), (1 R,2R)-N 1 , N2-dimethylcyclohexane-1 ,2- diamine (26.34mg, 0.190mmol) and cesium carbonate (607.03mg, 1 .85mmol The mixture was stirred at 120 C for 5 h. Reaction mixture was cooled to room temperature and then water and MTBE were added. After vigorously stirring, the layers were separated and the aqueous one was acidified to pH 2 with HCI 6N. The acidic solution was concentrated and purified by RP on C18 column [H20 (0.1 % HCOOH)/Acetonitrile=60/40] affording 6-methyl-3-(4-methyltriazol-2-yl)pyridine-2- carboxylic acid (p64, 139 mg, y= 69% yield) as a white solid. MS (mlz): 219.2 [MH]+.

In the meantime we’ve collected together some recent articles in this area about 27808-16-8 to whet your appetite. Happy reading!

Reference:
Patent; CHRONOS THERAPEUTICS LIMITED; MICHELI, Fabrizio; CREMONESI, Susanna; SEMERARO, Teresa; TARSI, Luca; GIBSON, Karl Richard; (116 pag.)WO2019/81939; (2019); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 151899-62-6, 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. 151899-62-6, name is 3-Iodo-1-trityl-1H-1,2,4-triazole, molecular formula is C21H16IN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

3-iodo-1-trityl -1H-1,2,4- triazole (300 mg),3-cyanophenyl boronic acid (101 mg), tetrakis triphenylphosphine palladium (79 mg), ethanol 2M aqueous sodium carbonate (1.5 mL) (1.0 mL) – toluene (1.5 mL) mixed solution of the mixture was stirred for 4 hours at 100 C. After cooling to room temperature, and separated the two layers.The aqueous layer was extracted with ethyl acetate, it was concentrated under reduced pressure and the organic layers were washed with. The residue was purified by column chromatography (silica gel cartridge, hexane: ethyl acetate = 88: 12-50: 50) to give the title compound (227 mg) as a colorless 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 3-Iodo-1-trityl-1H-1,2,4-triazole, hurry up and to see.

Reference:
Patent; TAISHO PHARMACEUTICAL COMPANY LIMITED; KONISHI, KAZUHIDE; KANUMA, KOSUKE; NAKAMURA, TOSHIO; AMADA, HIDEAKI; YAMAMOTO, SHUJI; KASHIWA, SHUHEI; MASUDA, SEIJI; OKADA, KUMIKO; KAWAMOTO, HIROSHI; (74 pag.)JP2015/78127; (2015); A;,
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. 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. 7411-23-6

Intermediate 11 -l-(2-methylallyl)-lH-l,2,4-triazole To 3,5-dibromo-lH-l,2,4-triazole (1.5 g, 6.61 mmol) in DMF (13 mL) was added sodium tert- pentoxide (0.728 g, 6.61 mmol) and the mixture was stirred for 10 min at rt under nitrogen atmosphere. 3-Bromo-2-methylprop-l-ene (0.667 mL, 6.61 mmol) was added and the mixture was stirred at 40C for 2 hours. The mixture was poured onto water and extracted with diisopropylether (2x). The organic phase was washed with water (2x), brine and dried over sodium sulfate. The solvents were evaporated to give the title compound as a liquid (1.70 g, 91%). GCMS (CI) m/z 281 [M+]. XH NMR (400 MHz, CDCI3) delta ppm 1.74 (d, 3 H) 4.69 (s, 2 H) 4.81 – 4.86 (m, 1 H) 5.05 (dd, 1 H).

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 7411-23-6

Reference:
Patent; ACTURUM LIFE SCIENCE AB; BESIDSKI, Yevgeni; YNGVE, Ulrika; PAULSEN, Kim; LINDE, Christian; MALMBORG, Jonas; WO2014/195322; (2014); 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. 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. 7411-23-6

1-(2-chloroethyl)piperidine hydrochloride (243 mg, 1.32 mmol), 3,5-dibromo-1H-1,2,4-triazole (250 mg, 1.1 mmol) and potassium carbonate (640 mg, 4.6 mmol) were added to DMF (5 mL) in a 25 mL round bottom flask. The reaction was then stirred for 18 h at 50 C under nitrogen. The solvent was removed in vacuo, water was added, and the product extracted with DCM (3 times). The organic phase was dried over a phase separator and the solvent removed in vacuo. The product was purified by silica column chromatography eluting with 0-10% MeOH in DCM to give [1-[2-(3,5-dibromo-1,2,4-triazol-1-yl)ethyl]piperidine (224 mg, 0.66 mmol, 60% yield)] as a yellow oil. UPLC-MS (ES+, Method A), 0.87 min, m/z 339.0 [M+H]+

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 3,5-Dibromo-1H-1,2,4-triazole ,and how the biochemistry of the body works.

Reference:
Patent; REDX PHARMA PLC; JONES, Clifford, D.; BUNYARD, Peter; PITT, Gary; BYRNE, Liam; PESNOT, Thomas; GUISOT, Nicolas, E.S.; (318 pag.)WO2019/145729; (2019); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 16681-70-2, New Advances in Chemical Research in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct 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.

[0427] To a stirred solution of (2S,4S)-4-amino-5-bipheny1-4-y 1-2-(3 -hydroxypropoxymethy l)pentanoic acid ethy Iester (18 mg, 47 flillOI) in DMF (0.3 mL), was added IH-1,2,3-triazole-4-carboxylic acid (5.3 mg, 47 f.tmol) and HATU (18mg, 47 f.tmol), followed by DIPEA(25 f.LL, 141 f.tmol). Themixture was stirred for 30 minutes, then concentrated underreduced pressure to yield crude Compound I, which was usedin the next step without purification.

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; 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

Application of 23579-79-5, 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. 23579-79-5, name is 3,5-Dibromo-1-methyl-1H-1,2,4-triazole, molecular formula is C3H3Br2N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

In a 50 mL pressure vial, 3,5-dibromo-1-methyl-1H-1,2,4-triazole (Int-41, 1.42 g, 5.89 mmol) was dissolved in DMF (12 mL) and potassium carbonate (1.36 mg, 9.82 mmol), followed by 3- chloro-5-methylphenol (700 mg, 4.91 mmol) were added. The vial was sealed, the reaction mixture was stirred for 15 h at 100 C. After cooling, it was concentrated in vacuo, the residue was purified by column chromatography (silica gel, 70 g, eluting with ethyl acetate / n-heptane, gradient 0: 100 to 25:75 v/v) to yield the title compound as white solid (1.37 g, 92%). 1H NMR (CDC13, 300 MHz): delta 2.37 (s, 3 H), 3.77 (s, 3 H), 6.99-7.02 (m, 1 H), 7.06-7.08 (m, 1 H), 7.11- 7.14 (m, 1 H). MS (ES+) m/z 302.0, 304.0, 306.0 [M+H, Br & CI isotopes] .

By the way, if you are interested in learning more fun chemistry with your kids, get your hands into one chemistry set now, and start enjoying the best part of chemistry: experiments about 3,5-Dibromo-1-methyl-1H-1,2,4-triazole.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BARTELS, Bjoern; BERCHTOLD, Stefan; GALLEY, Guido; GOERGLER, Annick; JAKOB-ROETNE, Roland; KRUMMENACHER, Daniela; LIMBERG, Anja; NEIDHART, Werner; RATNI, Hasane; REUTLINGER, Michael; RODRIGUEZ SARMIENTO, Rosa Maria; SCHNIDER, Christian; (309 pag.)WO2018/87018; (2018); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 4928-88-5, New Advances in Chemical Research 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. 4928-88-5, 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.

EXAMPLE 2 Preparation of methyl 1-(2,3,5-tri-O-Acetyl-beta-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate Using a Mixture of beta/alpha-1,2,3,5-Tetra-O-acetyl-L-ribofuranose A 2 L flask was charged with 80.5 g of triazolemethylester, the above dichloromethane solution of beta/alpha-1,2,3,5-Tetra-O-acetyl-L-ribofuranose, and 37 g of acetic anhydride at ambient temperature.The mixture was distilled at atmospheric pressure (bath temperature, 90° C.).When the pot temperature reached 85° C. and the distillation became very slow, vacuum was applied (up to 30 mbar) and the distillation was continued for 40 minutes at 90° C. (bath temperature) and then for another 40 minutes at 120° C. (bath temperature, the pot temperature reached 117° C.).The vacuum was released and 843 mg of triflic acid was slowly added.After the addition the vacuum was restored and the mixture was stirred at 115+-5° C. (pot temperature) for 4 h.Upon the completion of the reaction the mixture was cooled to 70° C. and to it was added 750 ML of 2B alcohol (ethyl alcohol).When a homogeneous solution was formed the mixture was cooled to 50° C. and held until heavy precipitation formed (seeding might be necessary).The mixture was then slowly cooled to -5° C. (bath temperature) in 2 h and held for at least 2 h.The solid was filtered, washed with 100 ML of cold 2B Alcohol (ethyl alcohol), and dried under vacuum at 50° C. for 17 h to give 192.7 g (75.1percent yield from L-ribose) of methyl 1-(2,3,5-tri-O-acetyl-beta-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate as an off-white solid.

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

Reference:
Patent; Dong, Zhiming; Zhang, Pingsheng; US2004/34213; (2004); 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. 27808-16-8, name is 4-Methyl-1H-1,2,3-triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Computed Properties of C3H5N3

A mixture of 33(430 mg, 1.00 mmol), 4-methyl-1H-1,2,3-triazole (100 mg,1.20 mmol) and K2CO3 (208 mg, 1.50 mmol) in DMF (4 mL)was stirred at 80C for 2 h. The mixture was quenched withwater at r.t. and extracted with EtOAc. The organic layer wasseparated, washed with water and saturated aqueous NaCl,dried over anhydrous MgSO4 and concentrated in vacuo(508.7 mg). The residue was purified by using preparativeHPLC (column: L-Column2 ODS 20 mm ID×150 mm L;mobile phase A: 0.1% TFA in water; mobile phase B: 0.1%TFA in acetonitrile; flow rate: 20 mL/min). The first elutingfactions (tR1) were concentrated to dryness, and washed withsaturated aqueous NaHCO3, extracted with EtOAc. The organic layer was separated, washed with water and saturatedaqueous NaCl, dried over anhydrous MgSO4 and concentratedin vacuo. The residue (42.7 mg) was crystallized from hexane-ethyl acetate to give 17 (34.4 mg, 0.072 mmol, 7.2%) asa white solid. 1H-NMR (300 MHz, DMSO-d6) delta: 1.04 (3H, s),1.37 (3H, s), 2.44 (3H, s), 4.87 (1H, d, J=8.3 Hz), 5.39 (1H, s),7.23-7.34 (2H, m), 7.48-7.58 (2H, m), 7.93 (1H, d, J=7.5 Hz),8.55 (1H, s), 8.88 (1H, d, J=0.8 Hz), 9.07 (1H, d, J=8.3 Hz),9.50 (1H, d, J=7.5 Hz). MS (ESI/APCI) m/z 476.2 [M+H]+.HPLC purity: 99.4%. mp 260C.

If you are hungry for even more, make sure to check my other article about 27808-16-8, the application of this compound in the production field has become more and more popular.

Reference:
Article; Mikami, Satoshi; Kawasaki, Masanori; Ikeda, Shuhei; Negoro, Nobuyuki; Nakamura, Shinji; Nomura, Izumi; Ashizawa, Tomoko; Kokubo, Hironori; Hoffman, Isaac Dylan; Zou, Hua; Oki, Hideyuki; Uchiyama, Noriko; Hiura, Yuuto; Miyamoto, Maki; Itou, Yuuki; Nakashima, Masato; Iwashita, Hiroki; Taniguchi, Takahiko; Chemical and Pharmaceutical Bulletin; vol. 65; 11; (2017); p. 1058 – 1077;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 288-36-8, New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 288-36-8, name is 1H-1,2,3-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.

EXAMPLE 1-C; 2-C2H-1.2.3-triazol-2-ylV5-methylbenzoic acid (1-5); A solution of 2-iodo-5-methylbenzoic acid (1-13, 4.0 g, 15.3 mmol) in DMF (10 mL) was treated with 1,2,3-triazole (2.1 g, 30.5 mmol), CsCO3 (9.95 g, 30.5 mmol), CuI (0.145 g, 0.76 mmol) and trans-N,N’-dimethylcyclohexane-l,2-diamine (0.43 g, 3.05 mmol). The mixture was heated at 120 0C for 10 min in a microwave reactor. The reaction was cooled to room temperature, diluted with water, and washed with EtOAc. The aqueous phase was acidified with IN HCl and extracted with EtOAc. The organic layer was dried over Na2SO4, filtered and concentrated. The residue was purified by gradient elution on SiO2 (0 to 10% MeOH in water with 0.1% AcOH) to give the faster eluting 2-(2H-l,2,3-triazol-2-yl)-5-methylbenzoic acid U5_, followed by the undesired regioisomer isomer, l-(2H-l,2,3-triazol-2-yl)-5-methylbenzoic acid (IzIA)- Data for M: 1HNMR (500 MHz, DMSO-d6) d 12.98 (br s , IH), 8.04 (s, 2H), 7.72-7.45 (m, 3H), 2.41 (s, 3H) ppm.

Therefore, this conceptually novel strategy might open impressive avenues to establish green and sustainable chemistry platforms.In my other articles, you can also check out more blogs about 1H-1,2,3-Triazole.

Reference:
Patent; MERCK & CO., INC.; WO2009/58238; (2009); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics