Day: August 20, 2021

Research speed reading in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 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. Application In Synthesis of 1H-[1,2,3]Triazole-4-carboxylic acid

Preparation 1 1-Trityl-1H-1,2,3-triazole-4-carboxylic Acid 1H-1,2,3-Triazole-4-carboxylic acid (20.0 g, 177 mmol) was combined with DMF (200 mL, 2.6 mol) and pyridine (100 mL, 1.2 mol), and the resulting mixture was cooled to 0 C. Triphenylmethyl chloride (54 g, 190 mmol) was added in portions and the mixture was stirred at room temperature for 24 hours. The resulting slurry was filtered and the filter cake was washed with water (2*200 mL) and air-dried yield an off white solid (60 g). The solid was slurried in THF (800 mL) at room temperature for 4 hours, then filtered. The filtrate was then concentrated by rotary evaporation, yielding a thick oil. EtOAc (500 mL) was added and the volume was reduced to 200 mL. The resulting thick slurry was filtered and dried to yield the title compound (35.5 g).

In conclusion, we affirm that quantitative kinetic descriptions of catalytic behavior continue to serve as an indispensable tool to navigate research efforts intended to model. Read on for other articles about 16681-70-2.

Reference:
Patent; Fleury, Melissa; Hughes, Adam D.; US2014/45906; (2014); 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.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. name: 3,5-Dibromo-1H-1,2,4-triazole

To a colorless solution of 3,5-dibromo-lH-l,2,4-triazole (lnt-1, 250 mg, 1.1 mmol, Eq: 1) and 3-iodooxetane (243 mg,1.32 mmol) in DMF (3 ml) was added K2CO3 (305 mg, 2.2 mmol). The vial was closed under Argon and stirred over night at 120C. The reaction mixture was diluted with 25 mL H2O and extracted with EtOAc (2 x 25 mL) and the organic layers were washed with sat NaCl (3 x 25 mL), dried over MgS04 and concentrated in vacuo. The title compound was isolated as a white solid (198 mg, 63.5 % yield). MS (ES+) m/z: 283.9 [(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; 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

Research speed reading in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 74733-90-7, name is 2-(4-Bromophenyl)-2H-1,2,3-triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. category: Triazoles

Step A) 2-[4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-2H-1,2,3-triazolePd(dppf)Cl2 (280 mg, 0.343 mmol) was added to a mixture of 2-(4-bromophenyl)-2H-1,2,3-triazole (255 mg, 1.14 mmol), 4,4,4′,4′,5,5,5′,5′-octamethyl-2,2′-bi-1,3,2-dioxaborolane (350 mg, 1.38 mmol), and potassium acetate (340 mg, 3.46 mmol) in 1,4-dioxane (10 mL). The reaction was heated to 80 C. and stirred at this temperature overnight. The reaction was allowed to cool to rt and was diluted with EtOAc (30 mL) and brine (30 mL). The mixture was filtered through celite, and the organic layer was separated from the filtrate. The aqueous layer was extracted with EtOAc (2×30 mL) and the organics were combined, dried (MgSO4), filtered and concentrated. The crude material was purified via flash chromatography using an Analogix SF15-12 g column and an eluent of EtOAc in n-heptane (0-10%) to afford the title compound as an orange solid (240.6 mg, 78.0%). MS (LCMS) m/z 272.4 (M+1). 1H NMR (400 MHz, CHLOROFORM-d) delta ppm 1.37 (s, 12H) 7.83 (s, 2H) 7.94 (d, 2H) 8.10 (d, J=8.59 Hz, 2H).

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 74733-90-7, and we look forward to future research findings.

Reference:
Patent; Pfizer Inc; US2012/232083; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference 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 13 A mixture of methyl 1,2,4-triazole-3-carboxylate (1.27 g, 0.01 mole) and beta-D-ribofuranosyl-1,2,3,5-tetraacetate (3.18 g, 0.01 mole) was melted and then 0.079 g of benzenesulfonic acid was added thereto. The reaction mixture was reacted for 5 hours, while maintaining the temperature of the reaction mixture at 95+-5° C. And then, the reaction mixture was crystallized with 300.8 nm of methanol to give 3.08 g of 1-(2,3,5-tri-O-acetyl-beta-D-ribofuranosyl)-1,2,4-triazole-3-carboxylic acid methyl ester (yield: 80percent).

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; Lee, Tai-Au; Park, Nam-Jin; Khoo, Ja-Heouk; Lee, Byung-Cheol; US2003/120064; (2003); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 178928-70-6, 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. 178928-70-6, name is 2-(2-(1-Chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl)-1H-1,2,4-triazole-3(2H)-thione, molecular formula is C14H15Cl2N3OS, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

1.1 Weigh 50 mg of the compound of formula I into a 10 mL sample vial, dissolve in 1.0 mL of diethylamine at room temperature and shake slightly until it is clear. When 5.0 mL of n-heptane was added dropwise, the solution appeared white turbid. After standing for 24 hours, light brown lump single crystals precipitated at the bottom of the bottle, and the color was darker. Filter out part of the single crystal, put it in a vacuum oven and dry for 6h, then the diethylamine solvate of the present invention can be obtained.

In the meantime we’ve collected together some recent articles in this area about 178928-70-6 to whet your appetite. Happy reading!

Reference:
Patent; East China University of Science and Technology; Li Zhong; Ren Guobin; Xu Xiaoyong; Hong Minghuang; Gong Chengyu; Hu Jian; (17 pag.)CN110272393; (2019); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 4928-87-4, 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. 4928-87-4, 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.

General procedure: The tail group amines Ar-NH2 (Ar a-d) (19.5 mmol,1.1 equiv) were added to a stirring solution of 1,2,4-triazole-3-carboxylic acid 12 (2.00 g, 17.7 mmol, 1.0 equiv) in dry DMF(30 mL) at room temperature. After 5 min, TBTU (6.0 g, 18.6 mmol,1.0 equiv) and DIPEA (11.0 mL, 61.9 mmol, 3.5 equiv) were added insequence. The resulting solution was stirred at room temperaturefor 16 h. After completion of the reaction, as indicated by TLC, DMFwas removed by rotary evaporation at 30 torr and 70 C. The crudematerial was purified by methods described in each individualentry.

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 1,2,4-Triazole-3-carboxylic acid is helpful to your research.

Reference:
Article; Chakraborty, Amarraj; Dou, Yali; Gibbons, Garrett S.; Grigsby, Sierrah M.; Lee, Young-Tae; Liao, Chenzhong; Mathew, Bini; Moukha-Chafiq, Omar; Nikolovska-Coleska, Zaneta; Pathak, Vibha; Reynolds, Robert C.; Schuerer, Stephan C.; Snowden, Timothy S.; Umeano, Afoma C.; European Journal of Medicinal Chemistry; vol. 189; (2020);,
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. 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

Sodium hydride (5.3 g, 220.85 mmol, 1.50 equiv) was added in portions to a stirred mixture of1H-1,2,3-triazole (10 g, 144.79 mmol, 1.00 equiv) in THF (500 mL) at 0 C under nitrogen. After1 hour 2-(trimethylsilyl)ethoxymethyl chloride (36 g, 235.76 mmol, 1.60 equiv) was added and theresulting solution was stirred for 12 h at room temperature. The reaction was quenched by water, extracted with ethyl acetate, dried over anhydrous sodium sulfate, and concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (1:10). This resulted in 10 g (28%) of the title compound as yellow oil. LC-MS (ES, mlz): 200 [M+H].

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 288-36-8, and we look forward to future research findings.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GENENTECH, INC.; BLAQUIERE, Nicole; BURCH, Jason; CASTANEDO, Georgette; FENG, Jianwen A.; HU, Baihua; STABEN, Steven; WU, Guosheng; YUEN, Po-wai; WO2015/25025; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 4928-87-4, 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, 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.

10.9 mg (0.077 mmol) of 1,2,4-triazole-3-carboxylic acid was dissolved in 5 ml of dichloromethane and 45.2 mg(0.119 mmol) of 2- (7-azobenzotriazole-Nu, Nu, N ‘, N’-tetramethyluronium hexafluorophosphate under ice bath was added 21.9 mg(0.216 mmol) of triethylamine,Stirring for 30min,30 mg of intermediate 121 (0.054 mmol) was added,Stir overnight at room temperature. TLC checkMeasurement,After the reaction,Add lml of saturated sodium bicarbonate solution,Stirring for 20min,Dispensing,The aqueous phase was extracted with dichloromethane,mergeThe organic phase,dry,Steamed in crude.The crude product was purified by preparative silica gel plate (methanol: dichloromethane = 1: 10)The target compound was 9 mg in 21%

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 Foreland Pharma Co., Ltd; Zhang, Xingmin; Wang, Ensi; Niu, Shengxiu; Guo, Jing; Dai, Zhuolin; Zheng, Nan; Ji, Qi; Li, Qinyan; Liang, Tie; (109 pag.)CN104411706; (2016); B;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 930-33-6, 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. 930-33-6, name is 1H-1,2,4-Triazol-3(2H)-one, molecular formula is C2H3N3O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

EXAMPLE 5 3-[6-Bromo-2-fluoro-3-(5-oxo-1,5-dihydro-[1,2,4]triazol-4-ylmethyl)-phenoxy]-5-chloro-benzonitrile (I-8) Ar=3-chloro-5-cyano-phenyl A solution of A-2d (200 mg, 0.477 mmol), 2,4-dihydro-[1,2,4]triazol-3-one (10, CASRN 930-33-6, 0.040 g, 1.0 eq), K2CO3 (0.13 g, 2.0 eq), and KI (0.008 g, 0.1 eq) and MeCN (1.5 mL) was heated to 85 C. for 2 h and then cooled to RT. The reaction mixture was diluted with 10% MeOH/DCM, and washed sequentially with water and brine. The organic extracts were evaporated and the crude product purified by SiO2 chromatography eluding with a MeOH/DCM gradient (3-10% MeOH) to afford 0.020 g (10%) of 1-8 as a white solid.

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-1,2,4-Triazol-3(2H)-one.

Reference:
Patent; Roche Palo Alto LLC; US2009/12034; (2009); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 16681-65-5, 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. 16681-65-5, name is 1-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.

1-Methyl-1H-1,2,3-triazole was prepared according to the literature reference WO2008/98104. To a 2 L flask containing 1-methyl-1H-1,2,3-triazole (9 g, 108.3 mmol) was added THF (1500 mL) and the solution was cooled to -40 C. To this colorless homogeneous solution was added n-butyllithium (2.5 M in hexanes, 45 mL, 112.5 mmol) dropwise which immediately afforded a dark brown viscous mixture. The mixture was kept between -10 to -20 C. for 60 minutes, then a THF solution of 2,4-dimethylthiazole-5-carbaldehyde (17.2 g, 121.8 mmol in 200 mL THF) was introduced via cannula. Once the aldehyde was added the reaction was allowed to warm to room temperature. After 3 hours, the reaction was quenched by pouring it into a saturated solution of aqueous NH4Cl. The aqueous portion was extracted with EtOAc in portions, 7*400 mL. The combined organics were washed with brine, dried over MgSO4, filtered and concentrated to dryness to give a brown oil. Chromatography on silica gel (10% acetone-DCM increasing to 50% acetone and increasing to 10% MeOH-DCM) provided the title compound as an amber solid.

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 1-Methyl-1H-1,2,3-triazole is helpful to your research.

Reference:
Patent; JOHNSON & JOHNSON; LEONARD, KRISTI A.; BARBAY, KENT; EDWARDS, JAMES P.; KREUTTER, KEVIN D.; KUMMER, DAVID A.; MAHAROOF, UMAR; NISHIMURA, RACHEL; URBANSKI, MAUD; VENKATESAN, HARIHARAN; WANG, AIHUA; WOLIN, RONALD L.; WOODS, CRAIG R.; FOURIE, ANNE; XUE, XIAOHUA; CUMMINGS, MAXWELL D.; MCCLURE, KELLY; TANIS, VIRGINIA; US2015/111870; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics