Tag: M.W:100-200

Application 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.

0867] lH-1,2,3-triazole-5-carboxylic acid (15.3 mg, 135f.tmol) andHATU (51.4mg, 135 fJ.mol)weremixedinDMF (4mL) and stirred at room temperature for 15 minutes. (2S,4S)-4-Amino-2-(1-amino-l-methylethyl)-5-( 5′-chloro-2′-fluorobiphenyl-4-yl)pentanoic acid ethyl ester (50 mg, 123 f.tmol)and DIPEA (64 f.LL, 369 f.tmol) were added. The resultingsolution was stirred at room temperature for 15 minutes, atwhich point LC/MS showed reaction completion. The solventwas removed in vacuo and the crude residue was diluted inEtOH (4 mL). A solution of IN LiOH (983 f.LL, 983 f.tmol) inwater was then added. The resulting solution was stirred at60 C. for 2 days, at which point LC/MS showed reactioncompletion. The solvent was removed in vacuo and the cruderesidue was purified by preparative HPLC to yield the titlecompound (4.2mg) as a TFA salt. MS rn/z [M+Ht calc’dforC23H25ClFN50 3 , 474.16. found 474.2.

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-4-carboxylic acid.

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

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.202931-88-2, name is 1-Methyl-1H-1,2,3-triazole-5-carbaldehyde belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Safety of 1-Methyl-1H-1,2,3-triazole-5-carbaldehyde

6-bromo-4-chloro-2-methoxy-3 – (4 – (trifluoromethyl) benzyl) quinoline (1.45 g, 3.37 mmol, Intermediate 10: step d) comprises that the flask, THF (25 was added to mL), the solution was cooled to -75 .n-BuLi (dropwise 2.5 M, 1.3 mL, 3.25 mmol )in hexane.After 2 minutes, 3 mL of THF 1 -methyl -1H-1,2,3-triazole-5-carbaldehyde (580 mg, 5.22 mmol, Intermediate 18) was introduced.The reaction mixture was warmed to -20 over 45 minutes and, at this time the reaction NH4was quenched with aqueous solution of Cl.Extract the aqueous portion with EtOAc (5 × 40 mL), washing the combined organics with brine, MgSO4dried over, filtered and concentrated.Silica gel (5% CH3CN-DCM, 30% CH3by chromatography on increased to CN + 2% MeOH), to give the title compound as a pale yellow non-crystalline solid.

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

Reference:
Patent; Janssen Pharmaceuticals N.V; Leonardo, Christi.A.; Barvei, Kent; Edward, James P.; Gloita, Kevin D.; Kummer, David .A.; Maharoof, Umar; Nishimura, Rachael; Urbanski, Mode; Venkatesan, Hariharan; Wang, Ai Hua; Olin, Ronald L.; Woods, Craig; Fourier, Anne; Shu, Jih; Cumings, Maxwell D.; (86 pag.)KR2016/68948; (2016); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 3179-31-5, New Advances in Chemical Research in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic,A common heterocyclic compound, 3179-31-5, name is 1H-1,2,4-Triazole-3-thiol, molecular formula is C2H3N3S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

Example 28 2,4-Difluoro-alpha-{[(1,2,4-triazol-3-yl)sulfanyl]methyl}-3-methoxy-beta-[(quinolin-5-yl)amino)-alpha-(trifluoromethyl)benzeneethanol 200 mg(0.47 mmmol) {[2,4-difluoro-3-methoxyphenyl][2-(trifluoromethyl)oxiranyl] methyl}-2-methylquinolin-5-amine (example 9) are dissolved in 2.0 ml DMF. 307 mg (0.94 mmol) Caesium carbonate are added followed by 190 mg (1.89 mmol) 3-mercapto-1,2,4-triazole. The mixture is vigorously stirred at ambient temperature for 4 hours. The reaction mixture is partitioned between ethyl acetate and water. The organic phase is washed with water and brine and evaporated. Flash chromatography on silica gel (acetone in hexane 10% to 50%) yields 66 mg of the title compound as one single diastereomer. 1H-NMR (DMSO d6); delta = 2.57 (s, 3H), 3.35 (d, 1 H), 3.67 (d, 1H), 3.81 (s, 3H), 5.31 (d, 1H), 6.29 (d, 1H), 6.33 (d, 1 H), 7.06 (dd, 1 H), 7.14 (d, 1H), 7.35 (d, 1H), 7.36 (t, 1H), 8.38 (s, 1H), 8.45 (d, 1 H).

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

Reference:
Patent; Bayer Schering Pharma Aktiengesellschaft; AstraZeneca AB; EP1878717; (2008); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 16681-70-2, New Advances in Chemical Research in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic,A common heterocyclic compound, 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.

[0814] 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 (20 mg) as a TFA salt. MS m/z [M+Hrcalc’d for C27H31CIFN50 4 , 544.21; found 544. Half of thecrude product was used in the next step without purification.

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-4-carboxylic acid is helpful to your research.

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

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. 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. Recommanded Product: 1,2,4-Triazole-3-carboxylic acid

A mixture of l-(7-Amino-5-(-8-azabicyclo[3.2.1]octan-3-yl)-3-(6-phenylpyridin-3- yl)pyrazolo[l,5-a]pyrimidin-6-yl)ethanone (131.4mg, 0.30 mmol), N2H4.H2O (150 ul, 3.0 mmol) in NMP (10 ml) was heated first at 100C for 30 min and then at 200C for 60 min under microwave condition. The mixture was put on rotovap and concentrated at 60C for 2h to remove excess N2H4.H20. lH-l,2,4-triazole-3-carboxylic acid (101.7 mg, 0.90 mmol), EDC (229 mg, 1.20 mmol), HOBt (121.5 mg, 0.90 mmol) and DIEA (521.6 uL, 3.0 mmol) were then added and the mixture was stirred at room temperature for lh. Purification with prep-LC pro ided (( 1 R,3 s,5 S)-3 -(3 -methyl-6-(6-phenylpyridin-3 -yl)- 1 H-dipyrazolo [1,5- a:4′,3′-e]pyrimidin-4-yl)-8-azabicyclo[3.2.1]octan-8-yl)(4H-l,2,4-triazol-3-yl)methanone.

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; MERCK SHARP & DOHME CORP.; MENG, Zhaoyang; PATEL, Mehul, F.; SIDDIQUI, M. Arshad; REDDY, Panduranga Adulla, P.; NAN, Yang; WO2013/16164; (2013); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 252742-72-6, 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. 252742-72-6, name is 3-(Chloromethyl)-1H-1,2,4-triazol-5(4H)-one, molecular formula is C3H4ClN3O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

13.35 g (100 mmol) of 3-chloromethyl-1,2,4-triazolin-5-one and 50 ml of THF were added to the reaction flask, stirred well, 220ml of 1mol / L sodium hexamethyldisilazane in tetrahydrofuran solution was added, cooled to -5 ° C, a solution of dibenzylphosphoryl chloride in tetrahydrofuran (32.6 g of dibenzylphosphoryl chloride dissolved in 50 ml of tetrahydrofuran) was slowly added dropwise, after the drop wise addition, the reaction was continued to stir, TLC monitoring reaction endpoint. 300ml saturated sodium bicarbonate solution and 300 ml of isopropyl ether was added to the reaction solution, Stirred for 15min, liquid separation, organic phase was washed with a saturated aqueous solution of sodium chloride and dried over anhydrous sodium sulfate, filtered , filtrate was concentrated to dryness , dried in vacuo to give a white solid of 35.84g, the yield was 91percent.

We very much hope you enjoy reading the articles and that you will join us to present your own research about 252742-72-6, Happy reading!

Reference:
Patent; Shandong New Age Pharmaceutical Co., Ltd.; Zhao Zhiquan; Bai Wenqin; Wang Youguo; Sun Xiuling; Dai Shaogang; (7 pag.)CN104650143; (2018); B;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 103755-58-4, 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. 103755-58-4, name is (1-Phenyl-1H-1,2,3-triazol-4-yl)methanol, 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: Into a round bottom flask was added 5.71mmolof triazole type 12 or 21a in 50mL of dry THF, 17.13mmolof sodium hydride and 57.1mmolof alkyl bromide. The mixture was heated to reflux, and reaction progress was monitored by TLC. Subsequently, the solvent was evaporated and the mixture was extracted with ethyl acetate, washed with distilled water (3×100mL) and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, and the product was purified via silica-gel column chromatography using a gradient mixture of hexane-ethyl acetate, to afford the pure derivatives 14a-g and 23a-b.

I am very proud of our efforts over the past few months and hope to (1-Phenyl-1H-1,2,3-triazol-4-yl)methanol help many people in the next few years.

Reference:
Article; Gonzaga, Daniel; Senger, Mario Roberto; Da Silva, Fernando De Carvalho; Ferreira, Vitor Francisco; Silva Jr., Floriano Paes; European Journal of Medicinal Chemistry; vol. 74; (2014); p. 461 – 476;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 16681-67-7, 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. 16681-67-7, name is 4-Bromo-2-methyl-2H-1,2,3-triazole, molecular formula is C3H4BrN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

4H-[l,2,4]triazolo[4,3-a][l,5]benzodiazepine, 5,6-dihydro-(4R)-l,4-dimethyl-8-(2- methyl- 2H-l,2,3-triazole-4-yl)-6-(4-chloro-phenyl) (Compound 48). A mixture of 4-R-4H- [l,2,4]triazolo[4,3-a][l,5]benzodiazepine, 5,6-dihydro-l,4-dimethyl-8-(4,4,5,5- tetramethyl-1.3.2- dioxaborolan-2-yl)-6-(4-chloro-phenyl) (200 mg, 0.44 mmol), 4-bromo-2-methyl-2H-1.2.3- triazole (72 mg, 0.44 mmol), tetrakis(triphenylphosphine)palladium(0) (51 mg) and potassium carbonate (243 mg, 1.76 mmol) in mixed solution of tetrahydrofuran (10 mL) and water (2 mL) was heated at 100C for 30 minutes under microwave (pressure: 17.2 bar, equipment power : 150W). The reaction mixture was diluted with ethyl acetate (50 mL), washed by brine (20 mL x 3), dried over anhydrous sodium sulfate and then filtered. The filtrate was concentrated and the residue was purified by column chromatography (silica gel,dichloromethane/methanol = 10:1) to afford 4-R-4H-[ 1,2,4] triazolo[4,3-a][l,5]benzodiazepine, 5,6-dihydro-l,4-dimethyl-8-(2-methyl-2H-l,2,3-triazole-4-yl)-6-(4-chloro-phenyl) as a white solid (80 mg, 44.5 %).

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 4-Bromo-2-methyl-2H-1,2,3-triazole.

Reference:
Patent; CONSTELLATION PHARMACEUTICALS, INC.; ALBRECHT, Brian, K.; GEHLING, Victor, S.; HEWITT, Michael, C.; TAYLOR, Alexander, M.; HARMANGE, Jean-Christophe; WO2012/151512; (2012); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 15988-11-1, 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. 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 for the synthesis oftriazolo[1,2-a]indazole-trione (1a-g) and2H-indazolo[2,1-b]phthalazine-triones (2a-g)To a well-ground mixture of arylaldehyde (1 mmol), dimedone(0.140 g, 1 mmol) and 4-phenylurazole (0.177 g, 1 mmol) or2,3-dihydrophthalazine-1,4-dione (0.162 g, 1 mmol), was added[Et3N-SO3H]HSO4[(0.028 g, 0.1 mmol) for the preparation of1a-gor (0.042 g, 0.15 mmol] for the synthesis of2a-g}. Theobtained mixture was firstly stirred magnetically at 90C, andafter solidification of the reaction mixture, it was stirred with asmall rod at same temperature. After the reaction was completed(as observed by TLC), the reaction mixture was cooled to roomtemperature, water (2 mL) was added, stirred for 3 min, andfiltered. The solid residue was recrystallized from EtOH/H2O(4/1) to give the pure product.

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 15988-11-1.

Reference:
Article; Zare, Abdolkarim; Masihpour, Fatemeh; Phosphorus, Sulfur and Silicon and the Related Elements; vol. 191; 8; (2016); p. 1160 – 1165;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 13273-53-5, 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. 13273-53-5, name is 4-Bromo-1-methyl-1H-1,2,3-triazole, molecular formula is C3H4BrN3, 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 4-bromo-1-methyl-1H-1,2,3-triazole (5 g, 30.87 mmol), tert-butyl prop-2-enoate (11.9 g, 92.85 mmol), palladium acetate (1.1 g, 4.90 mmol), tri-o-tolylphosphane (1.9 g, 6.24 mmol) and triethylamine (4.7 g, 46.45 mmol) in N,N-dimethylformamide (50 mL, 646.09 mmol) was stirred for 12 h at 110 C. The resulting mixture was cooled to room temperature and then diluted with water. The resulting solution was extracted with ethyl acetate, dried with anhydrous sodium sulfate. After filtration, the filtrate was concentrated under vacuum. The residue was purified by flash chromatography on a silica eluted with ethyl acetate/petroleum ether (3/2) to afford tert-butyl (2E)-3-(1-methyl-1H-1,2,3-triazol-4-yl)prop-2-enoate (3.6 g, 17.23 mmol) as a yellow solid. LCMS (ESI) [M+H]+=210

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 13273-53-5.

Reference:
Patent; Genentech, Inc.; Chan, Bryan; Drobnick, Joy; Gazzard, Lewis; Heffron, Timothy; Liang, Jun; Malhotra, Sushant; Mendonca, Rohan; Rajapaksa, Naomi; Stivala, Craig; Tellis, John; Wang, Weiru; Wei, BinQing; Zhou, Aihe; Cartwright, Matthew W.; Lainchbury, Michael; Gancia, Emanuela; Seward, Eileen; Madin, Andrew; Favor, David; Fong, Kin Chiu; Hu, Yonghan; Good, Andrew; US2018/282282; (2018); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics