Triazoles

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, This compound has unique chemical properties. The synthetic route is as follows., Recommanded Product: 1H-[1,2,3]Triazole-4-carboxylic acid

1,2,3-Triazole-4-carboxylic acid (14 mg, 124 mumol), DIPEA (86.3 muL, 496 mumol) and HATU (47.1 mg, 124 mumol) were combined in DMF (0.2 mL) and stirred for 5 minutes at room temperature. This was then combined with (2S,4R)-4-amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid benzyl ester (50 mg, 120 mumol). The resulting mixture was stirred for 15 minutes and the reaction was quenched with AcOH. The product purified by preparative HPLC and lyophilized to yield the title compound (13 mg; purity 95%). MS m/z [M+H]+ calc’d for C29H30N4O4, 499.23. found 499.4.

According to the analysis of related databases, 16681-70-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; THERAVANCE, INC.; US2012/213806; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 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

3,5-dibromo-1H-1,2,4-triazole (419 mg, 1.85 mmol) was added to a solution of phenylboronic acid (300 mg, 2.46 mmol), pyridine (0.2 mL, 2.46 mmol), copper(II) acetate (335 mg, 1.85 mmol) and 3 A molecular sieves in dry DCM (8 mL) and stirred at 25 C overnight. Upon completion monitored by LC/MS, sat. NH4Cl (20 mL) was added to the reaction mixture which was then washed with water, the organic layers were then combined and concentrated. The crude product was purified by flash column chromatography eluting with 15-50% EtOAc in Pet. Ether to give 3,5-dibromo-1-phenyl-1,2,4-triazole (454 mg, 1.50 mmol, 60% yield). LC-MS (ES+, Method A): 1.74 min, m/z 304.0 [M+H]+

The synthetic route of 7411-23-6 has been constantly updated, and we look forward to future research findings.

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

Synthetic Route of 16681-70-2, The chemical industry reduces the impact on the environment during synthesis 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, I believe this compound will play a more active role in future production and life.

EXAMPLE 3 4,5-Dibromo-1H-1,2,3-triazole STR12 To a solution of 140 g (1.32 moles) of sodium carbonate in 650 ml of water was added 75 g (661 mmoles) of 1H-1,2,3-triazole-4-carboxylic acid. The resulting solution was subjected to the dropwise addition of 208 g (1322 mmoles) of bromine and then stirred overnight at room temperature. After cooling to 0 C., the reaction was adjusted to pH 4 with 12N hydrochloric acid causing precipitation of 147 g (98%) of 4,5-dibromo-1-H1,2,3-triazole as a white solid. The structure was confirmed by n.m.r. and I.R.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 1H-[1,2,3]Triazole-4-carboxylic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Stauffer Chemical Company; US4596596; (1986); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 252742-72-6,Some common heterocyclic compound, 252742-72-6, name is 3-(Chloromethyl)-1H-1,2,4-triazol-5(4H)-one, molecular formula is C3H4ClN3O, 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.

A mixture of Example 87D (0.05 g, 0.126 mmol) and N-ethyl-N-isopropylpropan-2-amine (0.132 ml, 0.757 mmol) in Nu,Nu-dimethylformamide (1 mL) was treated with Example 637A (0.020 g, 0.151 mmol) and the reaction was stirred at room temperature for 3 hours. Additional N-ethyl-N- isopropylpropan-2-amine (0.05 mL) and additional Example 637A (0.010 g, 0.076 mmol) were added and the mixture was stirred 3 hours longer. The reaction mixture was directly purified by reverse phase HPLC on a Phenomenex Luna C8(2) 5 um IotaOmicronthetaAlpha AXIA column (30 mm x 75 mm) eluting with a gradient of 10-70percent acetonitrile in 0.1 percent ammonium acetate/water to afford the title compound. lH NMR (500 MHz, DMSO-d6) delta ppm 2.44 – 2.52 (m, 2H), 2.64 (t, J = 5.8 Hz, 2H), 3.14 (q, J = 2.7 Hz, 2H), 3.40 (s, 2H), 3.73 (s, 3H), 6.19 (d, J = 2.1 Hz, 1H), 6.44 – 6.51 (m, 1H), 7.02 (d, J = 4.9 Hz, 1H), 7.14 – 7.32 (m, 3H), 8.18 (d, J = 4.9 Hz, 1H), 1 1.24 (s, 1H), 1 1.30 – 1 1.39 (m, 1H), 1 1.77 (d, J = 2.2 Hz, 1H). MS (ESI+) m/z 421.1(M+H)+.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 3-(Chloromethyl)-1H-1,2,4-triazol-5(4H)-one, its application will become more common.

Reference:
Patent; ABBVIE INC.; ABBVIE PHARMACEUTICAL TRADING (SHANGHAI) CO., LTD.; TONG, Yunsong; BRUNCKO, Milan; CLARK, Richard F.; CURTIN, Michael L.; FLORJANCIC, Alan S.; FREY, Robin R.; GONG, Jianchun; HANSEN, Todd M.; JI, Zhiqin; LAI, Chunqiu; MASTRACCHIO, Anthony; MICHAELIDES, Michael; MIYASHIRO, Juliem; RISI, Roberto M.; SONG, Xiaohong; TAO, Zhi-fu; WOODS, Keith W.; ZHU, Guidong; PENNING, Thomas; SOUERS, Andrew; GOSWAMI, Rajeev; IQUTURI, Omprakash Reddy; DABBEERU, Madhu Babu; WO2014/139328; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 4928-88-5, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 4928-88-5 name is Methyl 1H-1,2,4-triazole-3-carboxylate, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

In a 250 mL four-necked flask equipped with a mechanical stirrer, thermometer and distillation apparatus, 100.0 g of tetraacetyl ribose was added and heated to 100 ¡ã C in an oil bath.After the tetraacetyl ribose is completely melted into a transparent liquid, the stirring is started.40.0 g of methyl 1,2,4-triazolecarboxylate was added, and the two materials were uniformly mixed.Add 1.4g of elemental iodine, continue to raise the temperature to 115 ¡ã C, and keep warm for 2 hours.Then, vacuuming was started, and by-product acetic acid was distilled off; after 1 hour, the reaction was stopped, and the mixture was cooled to 70 ¡ã C or lower, 100 mL of methanol was taken, and the mixture was added to the flask, and the mixture was stirred to uniformly dissolve the material, and poured into a beaker. Allow to cool to room temperature,Precipitate solids, filter, wash, dry,Ribavirin intermediate[1-(2,3,5-Tri-O-acetyl-beta-D-ribofuranosyl)-1H-1,2,4-triazole-3-carboxylic acid methyl ester], yield 82percent (Based on tetraacetyl ribose, the same below.)

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Methyl 1H-1,2,4-triazole-3-carboxylate, and friends who are interested can also refer to it.

Reference:
Patent; Henan Academy Of Sciences High Technology Research Center; Zhang Jiaxiang; Guo Xiaozhan; Chen Tiantian; Wang Huafen; Ren Zhiyong; Gong Wei; Fu Yang; Jiang Lei; (10 pag.)CN109336937; (2019); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 6523-49-5, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 6523-49-5 name is 4-(1,2,4-Triazol-1-yl)aniline, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

N’ – [5 -(3 -Chloro-propoxy)-2-cyano-4-methyoxy-phenyl] -N,N-dimethyl- formamidine (WO03055491, 580 mgs)5 4-(l,2,4-triazolyl)aniline (314 mgs) and AcOH(4 mL) were heated to 90 for 1 hr before cooling. The oil was concentrated and the resultant slurry dissolved in MeOH, sonicated and the resultant white powder filtered and dried to produce the title compound (765 mg). 1H NMR delta 9.65 (s, IH), 9.25 (s, IH), 8.5 (s, IH), 8.23 (s, IH), 8.02 (d, 2H, J9Hz ), 7.89 (s, IH), 7.87 (d, 2H, J=9), 7.24 (s, IH), 4.28 (t, 2H, J=6), 3.95 (s, 3H), 3.83(t, 2H, J6Hz), 2.27 (q, 2H, J6Hz); LC-MS rt 2.13 m/z 411 ES+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 4-(1,2,4-Triazol-1-yl)aniline, and friends who are interested can also refer to it.

Reference:
Patent; ARROW THERAPEUTICS LIMITED; WO2007/80401; (2007); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 1001401-62-2, These common heterocyclic compound, 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, 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.

A mixture of 2-(2H-l,2,3-triazol-2-yl)benzoic acid (100 mg, 0.528 mmol) in SOCl2 (251.5 mg, 2.11 mmol) was stirred at RT for 0.5 h, then concentrated in vacuo. To a solution of the product from Step 3 (110 mg, 0.48 mmol) and Et3N (145.7 mg, 1.44 mmol) in DCM (1 mL) at 0 C was added a solution of the above residue in DCM (1 mL) dropwise. The resulting mixture was stirred at 0 C for 2 h, then quenched with water (1 mL) and extracted with DCM (2 mL x 3). The combined organic layers were washed with brine (2 mL), dried over Na2SC>4, filtered, and concentrated in vacuo. The residue was purified by prep-TLC (50% EtOAc in petroleum ether) to give the title compound as a oil. LRMS m/z (Mu+Eta) 400.0, 402.0 found, 400.1, 402.1 required.

Statistics shows that 2-(2H-1,2,3-Triazol-2-yl)benzoic acid is playing an increasingly important role. we look forward to future research findings about 1001401-62-2.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; LIVERTON, Nigel; LUO, Yunfu; (85 pag.)WO2016/100156; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 41253-21-8, name is Sodium 1,2,4-triazol-1-ide, A new synthetic method of this compound is introduced below., category: Triazoles

(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.

The synthetic route of 41253-21-8 has been constantly updated, 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

Reference of 956317-36-5, The chemical industry reduces the impact on the environment during synthesis 956317-36-5, name is 5-Methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid, I believe this compound will play a more active role in future production and life.

5-methyl-2- (2H-1,2,3-triazol-2-yl)Benzoic acid (2.03 g, 10 mmol)Was added to a 100 mL single-necked round bottom flask,Dried over anhydrous dichloromethane (20 mL)Sulfur chloride (15 mL, 200 mmol) was added slowly,And pyridine (0.15 mL, 2 mmol)The temperature was gradually raised to reflux for 3 hours.Stop the reaction,cool down,The solvent is slowly evaporated under reduced pressure,The resulting product was used directly in the next step.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 5-Methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Guangdong HEC Pharmaceutical Co., Ltd.; Jin, Chuanfei; Gao, Jinheng; Zhang, Yingjun; (39 pag.)CN106243052; (2016); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 1455-77-2, name is 3,5-Diamino-1,2,4-triazole, A new synthetic method of this compound is introduced below., Computed Properties of C2H5N5

A solution of 3-(dimethylamino)-1-phenylpropan-1-one hydrochloride 9 (9.36 mmol) and diaminotriazole 10 (9.36 mmol) in 20 mL of acetic acid was heated to reflux for 6 h. The reaction mixture was cooled and the solvent evaporated in vacuo to furnish a mixture of desired product 12 (minor) and 5-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine (major). The crude mixture was taken to the next step without any further purification and it was treated with N-bromosuccinimide (14.03 mmol) in ethanol (20 mL) under reflux for 5 h to promote the oxidation of the dihydrotriazolopyrimidine. The reaction mixture was cooled, and the solvent was evaporated in vacuo to yield a pale-yellow solid. The crude compound was purified by flash chromatography on silica gel using as eluent a gradient of EtOAc (0-50percent) to produce the desired compound 12 as white solid (adapted from 2). Yield: 29percent (0.57 g). 1H NMR (600 MHz, DMSO-d6) delta 9.07 (d, J = 6.9 Hz, 1H), 8.21 ? 8.19 (m, 2H), 7.72 (d, J = 6.9 Hz, 1H), 7.56 (s, 3H). HRMS-ESI (+) m/z calculated for C11H10N5, 212.0936 [M+H]+; found: 212.0941

The synthetic route of 1455-77-2 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Ribeiro, Carlos J.A.; Kankanala, Jayakanth; Xie, Jiashu; Williams, Jessica; Aihara, Hideki; Wang, Zhengqiang; Bioorganic and Medicinal Chemistry Letters; vol. 29; 2; (2019); p. 257 – 261;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics