Month: April 2021

Synthetic Route of 7411-23-6,Some common heterocyclic compound, 7411-23-6, name is 3,5-Dibromo-1H-1,2,4-triazole, molecular formula is C2HBr2N3, 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.

Intermediate 4 3,5-Dibromo-l-methyl-lH-l,2,4-triazole To a solution of 3,5-dibromo-lH-l,2,4-triazole (1.0 g, 4.41 mmol) in DMF (9 mL) sodium tert- pentoxide (0.485 g, 4.41 mmol) was added and the mixture was stirred for 10 min at rt under nitrogen atmosphere, lodomethane (0.29 mL, 4.63 mmol) was added and the mixture was stirred at 40C for 2 hours. The mixture was poured onto water and extracted twice with diisopropylether. 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 solid (0.83 g, 78%).

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

Reference:
Patent; ACTURUM LIFE SCIENCE AB; BESIDSKI, Yevgeni; YNGVE, Ulrika; PAULSEN, Kim; LINDE, Christian; NORDVALL, Gunnar; MACSARI, Istvan; MALMBORG, Jonas; WO2014/195321; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 1455-77-2, name is 3,5-Diamino-1,2,4-triazole, belongs to Triazoles compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 1455-77-2, Safety of 3,5-Diamino-1,2,4-triazole

3,5-Diamino-1,2,4-triazole was dissolved in 66percent hydrofluoric acid aqueous solution. After short heating in a water bath and slow cooling, crystals of (HL)(H2L)(HF2)2F compound (I) were found.

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, 3,5-Diamino-1,2,4-triazole, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Goreshnik, Evgeny; Journal of Fluorine Chemistry; vol. 197; (2017); p. 94 – 99;,
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. 4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, A new synthetic method of this compound is introduced below., Product Details of 4928-87-4

A solution of 1H-1,2,4-triazole-3-carboxylic acid (0.072 g, 0.64 mmol), N- [(dimethylamino)(3H-[1 ,2,3]triazolo[4,5-b]pyridin-3-yloxy)methylene]-lambda/- methylmethanaminium hexafluorophosphate (0.243 g, 0.64 mmol) and lambda/-ethyl-lambda/- isopropylpropan-2-amine (0.205 mL, 1.17 mmol) in DMF (1.5 mL) was stirred for 15 minutes under argon. Finally, 3″-fluoro-3,2I:3l,4″-terpyridine-5′,6I-diamine (Intermediate 1 , 0.15 g, 0.53 mmol) in DMF (3 mL) was added and the mixture was stirred at room temperature for 20 hours. The solvent was evaporated and the crude mixture was purified by silica gel flash chromatography (90:10 dichloromethane/methanol) to give the title compound (0.070 g, 35% of yield). ESI/MS m/e: 377 ([M+H]+, C18H13FN8O).

The synthetic route of 4928-87-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; LABORATORIOS ALMIRALL, S.A.; WO2007/39297; (2007); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

7170-01-6, name is 3-Methyl-1H-1,2,4-triazole, belongs to Triazoles compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Application In Synthesis of 3-Methyl-1H-1,2,4-triazole

Example 41 b. l-(2-methoxy-4-nitrophenyl)-3-methyl-lH-l,2,4-triazoleA mixture of 3-methyl-lH-[l,2,4]triazole (2.4 g, 29.21 mmol), l-fluoro-2-methoxy-4- nitrobenzene (5.0 g, 29.21 mmol) and potassium carbonate (8.06 g, 58.42 mmol) in DMF (50 mL) was heated overnight at 85C in a pressure vessel. The reaction mixture was cooled to room temperature and concentrated under reduced pressure. The residue was suspended in water and the mixture extracted with dichloromethane. The organic extracts were combined, washed with brine, dried over anhydrous Na2SO4, filtered and concentrated. The residue was dissolved in dichloromethane (50 mL) and hexane was added in small portions until the solution become slightly turbid. The turbid solution was left at room temperature. The precipitation was collected by filtration, washed with hexane to give 2.5 g of title compound (37 % Yield).1U NMR (400 MHz, CHLOROFORM-J) delta ppm 2.51 (s, 3 H) 4.10 (s, 3 H) 7.90 – 8.06 (m, 2 H) 8.10 (d, I H) 8.87 (s, I H)

The synthetic route of 7170-01-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ASTRAZENECA AB; LO-ALFREDSSON, Yvonne; PAULSEN, Kim; RAKOS, Laszlo; ROTTICCI, Didier; WALDMAN, Magnus; WO2010/132015; (2010); 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. 288-36-8, name is 1H-1,2,3-Triazole, A new synthetic method of this compound is introduced below., Recommanded Product: 288-36-8

To a solution of 2-iodobenzoic acid (3.0 g, 12.1 mmol) in DMF was added 1,2,3- triazole (1.5 g, 21.7 mmol), Cs2CO3 (7.1 g, 21.7 mmol), Cul (114 mg, 0.6 mmol), and trans-N,N?dimethylcyclohexane- 1 ,2-diamine (310 mg, 2.2 mmol). After heating at 120 C for 10 mm in amicrowave reactor, the mixture was cooled to room temperature, diluted with EtOAc, and filtered through Celite. The filtrate was concentrated in vacuo and the crude residue was purified by silica gel chromatography (MeOH in DCM with 0.1% AcOH) to give Intermediate N as the faster eluting isomer. ?H NMR (DMSO-d6, 500MHz) oe 13.05 (brs, 1 H), 8.12 (s, 2H), 7.8 1-7.52 (m, 4H).

The synthetic route of 288-36-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; REGER, Thomas, S.; ROECKER, Anthony, J.; (0 pag.)WO2016/85783; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 626248-56-4,Some common heterocyclic compound, 626248-56-4, name is 3-(2H-1,2,3-Triazol-2-yl)aniline, molecular formula is C8H8N4, 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 tert-butyl (1 S,2R)-2-(3-bromo-4- cyanophenylamino)cyclohexylcarbamate (150 mg, 0.380 mmol), 3-(2H-l,2,3-triazol-2- yl)aniline (100 mg, 0.625 mmol), BINAP (40 mg, 0.064 mmol), Pd(OAc)2 (25 mg, 0.11 mmol) and K2C03 (150 mg, 1.08 mmol) in dioxane (3 mL) was degassed with Ar, then was stirred at 100 C for 4 h. EtOAc and water were added. The organic phase was separated, washed with IN HCl, then with 5% NaHC03, dried over Na2S04, concentrated in vacuo to give tert-butyl (lS,2R)-2-(3-(3-(2H-l,2,3-triazol-2-yl)phenylamino)-4- cyanophenylamino)cyclohexylcarbamate as a crude residue.

The synthetic route of 626248-56-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; PORTOLA PHARMACEUTICALS, INC.; JIA, Zhaozhong, J.; SONG, Yonghong; XU, Qing; KANE, Brian; BAUER, Shawn, M.; PANDEY, Anjali; WO2012/61418; (2012); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 288-36-8 as follows. COA of Formula: C2H3N3

Example 159: Preparation of 4,5-dibromo- IH-[1, 2,3 ItriazoleTo a solution of IH-[1, 2,3]triazole (1.26 ml, 21.7 mmol) in water (10 ml) at 50¡ãC, was added bromine (1.5 ml, 29 mmol). The reaction mixture was stirred at 50¡ãC for 1.5 hours. The white solid (2.375 g) was isolated via filtration and washed with water (5 ml). To the combined filtrates was added more bromine (1.5 ml, 29 mmol). The reaction mixture was stirred at room temperature for 20 hour. More white solid (1.83 g) was isolated via filtration and washed with water (5 ml). To the combined filtrates was added more bromine (1.5 ml, 29 mmol). The reaction mixture was stirred at room temperature for 20 hours. More white solid (375 mg) was isolated via filtration and washed with water (5ml). The white solids were combined and dried to give 4,5-dibromo- IH-[1, 2,3]- triazole (4.92 g, 93percent yield). M.p. 194.70C.

According to the analysis of related databases, 288-36-8, the application of this compound in the production field has become more and more popular.

Reference:
Patent; SYNGENTA LIMITED; WO2007/71900; (2007); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 60166-43-0, 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. 60166-43-0, name is 1,4-Dimethyl-1H-1,2,3-triazole belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below.

A mixture of 7-bromo-5-nitro-2H-isoquinolin-1-one (7.3, 1 g, 3.72 mmol, 1 equivalent), 1,4-dimethyltriazole (397 mg, 4.09 mmol, 1.1 equivalents), KOAc (1.82 g, 18.6 mmol, 5 equivalents), Pd(OAc)2 (83.5 mg, 372 mumol, 0.1 equivalent) and bis(1-adamantyl)butylphosphane (267 mg, 743 mumol, 0.2 equivalent) in 2-methylbutan-2-ol (100 mL) was purged with nitrogen 3 times. This reaction mixture was stirred at 120 C. for 12 hours under a nitrogen atmosphere. After this time, the reaction mixture was diluted with ethyl acetate (50 mL) then it was filtered. The filtrate was washed with brine (30 mL*3), dried over sodium sulfate and concentrated. This crude product was purified further by column chromatography (SiO2, dichloromethane/methanol 200/1 to 50/1) to give 7-(3,5-dimethyltriazol-4-yl)-5-nitro-2H-isoquinolin-1-one (7.4, 550 mg, 1.93 mmol, 51.8% yield) as a yellow solid; LCMS [M+1]: 286.2. 1H NMR (400 MHz, DMSO-d6) delta=11.96 (br s, 1H), 8.65-8.48 (m, 2H), 7.54 (br s, 1H), 6.97 (d, J=7.6 Hz, 1H), 3.99 (s, 3H), 2.28 (s, 3H)

The synthetic route of 1,4-Dimethyl-1H-1,2,3-triazole has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Mirati Therapeutics, Inc.; Marx, Matthew Arnold; Lee, Matthew Randolph; Galemmo, Robert Anthony; Bobinski, Thomas P.; US2018/265517; (2018); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

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. 288-36-8, name is 1H-1,2,3-Triazole, This compound has unique chemical properties. The synthetic route is as follows., Computed Properties of C2H3N3

Intermediate E: 2-(2H-l,2,3-triazol-2-yl)benzoic acid Int E Step 1 : 2-(2H-l,2,3-triazol-2-yl)benzoic acid (Int E) To a solution of 2-iodobenzoic acid (3.0 g, 12.1 mmol) in DMF was added 1,2,3-triazole (1.5 g, 21.7 mmol), Cs2C03 (7.1 g, 21.7 mmol), Cul (114 mg, 0.6 mmol), and trans-N,N’-dimethylcyclohexane- 1,2-diamine (310 mg, 2.2 mmol). After heating at 120 C for 10 min in a microwave reactor, the mixture was cooled to room temperature, diluted with EtOAc, and filtered through Celite. The filtrate was concentrated in vacuo and the crude residue was purified by silica gel chromatography (MeOH in DCM with 0.1% AcOH) to give Int E as the faster eluting isomer. 1H NMR (DMSO-d6, 500MHz) delta 13.05 (brs, 1 H), 8.12 (s, 2H), 7.81-7.52 (m, 4H).

According to the analysis of related databases, 288-36-8, the application of this compound in the production field has become more and more popular.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; REGER, Thomas, S.; ROECKER, Anthony, J.; WO2015/95111; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 288-36-8, 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. 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.

To a mixture of 2bromo441uorobenzoic acid (30 g, 137 mmol), cesium carbonate (89.26 g, 274 rnmol) and Cul (5.27 g, 27,4 mmol) in DMF (200 mL) were added NN?dimeLhyicyelohexanei,2diamine (3.7 mL,23.3 mmoi) and 1Hi,2,3-triazoie (18.92 g, 274mmoi). The resulting mixture was stirred at 110 C overnight, cooled, concentrated in vacuo and diluted with water (150 rnL). The aqueous layer was extracted with EtOAc (300 mL x 3). The aqueous layer was acidified with 2N HCI and extracted with EtOAc (300 rnL x 4). The combined organic layers were washed with brine (150 mL x 3), dried over Na2SO4, filtered and the filtrate concentrated in vacuo, The residue was purifIed by chromatography on silica gel(petroleum ether: EtOAc = 100: 1 5 : 1) to provide the title compound as a solid. LRMS m/z (M+H) 208.0 found, 208.0 required.

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, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott D.; LIVERTON, Nigel; LUO, Yunfu; SKUDLAREK, Jason; (79 pag.)WO2016/95204; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics