Category: 1001401-62-2

Application of 1001401-62-2,Some common heterocyclic compound, 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, molecular formula is C9H7N3O2, 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.

Step 6: (2-(2H-1 ,2,3-triazol-2-yl)phenyl)((2R,5R)-5-hydroxy-2-methylpiperidin-1-yl)methanone (6) A solution of (3R, 6R)-6-methylpiperidin-3-ol (5.31 g, 46.1 mmol), 2-(2H-1,2,3- triazol-2-yl)benzoic acid (10.5 g, 55.3 mmol), EDC (17.7 g, 92.0 mmol), 1-hydroxy-7- 30 azabenzotriazole (12.6 g, 92.0 mmol), triethylamine (19.3 mL, 138 mmol) in DMF (300 mL) was stirred at 50 C overnight, then diluted with saturated aqueous sodium bicarbonate and extracted 3x with ethyl acetate. The organics were washed with brine, dried over magnesium sulfate, filtered, and concentrated. The crude material was purified by silica gel gradient chromatography (0-100% ethyl acetate in hexanes), providing the titled compound as a pale yellow solid. LRMS m/z (M+H) 287.3 found, 287.1 required.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, its application will become more common.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; SKUDLAREK, Jason, W.; WO2015/88864; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

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. Recommanded Product: 1001401-62-2

To a solution of 2-(2H-1,2,3-triazol-2-yl)benzoic acid (500 mg, 2.65 mmol) in DMF (8 mL) was added HATU (1.51 g, 3.98 mmol) and DIEA (1.03 mg, 7.95 mmol). The resulting mixture was stirred at RT for 30 mins, and then tert-butyl hexahydropyrrolo[3,4-cjpyrrole- 2(1H)-carboxylate (562 mg, 2.65 mmol) was added. The resulting mixture was stirred at RT for2 h. The reaction mixture was filtered and the filtrate was concentrated in vacuo. The residue was purified by silica gel column chromatography (10% – 50% EtOAc in petroleum ether) to give the title compound as a oil. LRMS m/z (M+H) 384.2 found, 384.2 required.

The synthetic route of 2-(2H-1,2,3-Triazol-2-yl)benzoic acid has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; LIVERTON, Nigel; REGER, Thomas, S.; SKUDLAREK, Jason, W.; (50 pag.)WO2016/100162; (2016); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

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. SDS of cas: 1001401-62-2

j0814] To the title compound of step B (140 mg, 0.5 mmol) and intermediate A-i (113 g, 0.6 mmol) in DMF (4 mE) was added DIPEA (230 jt, 1.4 mmol) and HATU (155 g, 0.6 mmol). Upon completion of the reaction, purification was performed using Agilent prep method X to give the title compound (172 g, 74%). MS (ESI) mass calcd. for C2QH,8F3N70, 429.2; mlz found 430 [M+H]. 1H NMR (CDC13): 8.32 (s, 0.3H), 8.17 (s, 0.7H), 7.99-7.89 (m, i.5H), 7.88-7.77 (m, 1 .5H), 7.62-7.30 (m, 4H), 6.24-6.15 (m, 0.3H),4.86 (s, 0.7H), 4.76 (d, J=5.4 Hz, 0.3H), 4.45-4.23 (m, 1H),

The synthetic route of 2-(2H-1,2,3-Triazol-2-yl)benzoic acid has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Janssen Pharmaceutica NV; COATE, Heather R.; DVORAK, Curt A.; FITZGERALD, Anne E.; LEBOLD, Terry P.; PREVILLE, Cathy; SHIREMAN, Brock T.; (473 pag.)US2016/46640; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Electric Literature of 1001401-62-2,Some common heterocyclic compound, 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, molecular formula is C9H7N3O2, 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 the product from step 5 (50 mg, 0.17 mmoi), FIATU (95 mg, 0.25 mmol), TEA (0.3 mL) and 2-.(2fi-J,234riazoi-2y1)benzoic acid (34.8 mg, 0.18 mmoi) in DMF (2 mL) was stirred at RI for 9 hours under the N2 atmosphere. Then the mixture was poured into water(5 rnL x 3) and extracted with EtOAc (5 mL x 3). The combined organic layer was washed withbrine, dried over magnesium sulfate, filtered and concentrated in vacuo. The residue waspurified by Prep?HPLC to give the title compound (30 mg) as yellow oil, LRMS m/z (M¡ÂH)471.1 found, 471.1 required.

The synthetic route of 1001401-62-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME CORP.; LIVERTON, Nigel; KUDUK, Scott D.; BESHORE, Doug C.; MENG, Na; LUO, Yunfu; (127 pag.)WO2016/101119; (2016); 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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, This compound has unique chemical properties. The synthetic route is as follows., category: Triazoles

General procedure: A mixture of the primary amine, 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid 31 (0.33 g, 1.6 mmol), N,N-diisopropylethylamine(DIPEA, 2.5 mL, 14.7 mmol), and 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate(HATU, 0.91 g, 2.4 mmol) in DMF (3.2 mL) was stirredat room temperature for 17 h. The reaction was quenched by theaddition of water, and the mixture was extracted with EtOAc.The organic layer was washed with brine, dried over Na2SO4, filtered,and concentrated under reduced pressure. The resulting residuewas purified by preparative HPLC to obtain the title compound7a as a colorless solid (0.18 g, 28% over 2 steps).

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 1001401-62-2.

Reference:
Article; Futamura, Aya; Nozawa, Dai; Araki, Yuko; Tamura, Yunoshin; Tokura, Seiken; Kawamoto, Hiroshi; Tokumaru, Yuichi; Kakihara, Sora; Aoki, Takeshi; Ohtake, Norikazu; Bioorganic and Medicinal Chemistry; vol. 25; 20; (2017); p. 5203 – 5215;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 1001401-62-2, 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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, This compound has unique chemical properties. The synthetic route is as follows.

2-(2H-1,2,3-Triazol-2-yl)benzoic acid (0.02 g, 0.1 mmol), HOBt.H2O (0.022 g, 0.14 mmol), and EDC.HCl (0.027 g, 0.14 mmol) were added to a solution of N-ethyl-2-[1-(5-fluoropyridin-2-yl)-1H-pyrazol-3-yl]ethanamine (0.022 g, 0.09 mmol) prepared in Reference Example 10 in DMF (0.8 mL), followed by stirring at room temperature for 2 hours. An aqueous NaHCO3 solution was added to the reaction mixture, followed by extract with EtOAc. The solvent was distilled off under reduced pressure. The resulting residue was purified by column chromatography (HP-Sil: 10 g, hexane/EtOAc=80/20 to 0/100, KP-NH: 11 g, hexane/EtOAc=88/12 to 0/100), followed by washing with Et2O with stirring to give the titled compound (0.013 g, colorless solid). LCMS retention time: 5.54 min (Condition 1) MS (ESI pos.) m/z: 406 [M+H]+

The chemical industry reduces the impact on the environment during synthesis 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.

Reference:
Patent; TAISHO PHARMACEUTICAL CO., LTD.; Suzuki, Ryo; Futamura, Aya; Abe, Masahito; Kashiwa, Shuhei; Hattori, Nobutaka; Nozawa, Dai; Ohta, Hiroshi; Araki, Yuko; US2014/81025; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products 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.

Step 6: l-(3-(r(3i?,6i? -6-Methyl-l- (r2-(2H-l,2,3-triazol-2-vnphenyllcarbonvUpiperidin-3- yl”|oxy|phenyl)ethanol A solution of l-(3-(((3i?,6i?)-6-methylpiperidine-3-yl)oxy)phenyl)ethanol (0.020 g, 0.085 mmol), 2-(2H-l,2,3-triazol-2-yl)benzoic acid (0.024 g, 0.13 mmol), EDC (0.033 g, 0.17 mmol), 1 -hydroxy-7-azabenzotriazole (0.023 g, 0.17 mmol), and Hunig’s base (0.089 mL, 0.51 mmol) in DMF (1 mL) was stirred at 50 C overnight, then diluted with saturated aqueous sodium bicarbonate and extracted 2x with ethyl acetate. The combined organic fractions were washed with brine, dried over magnesium sulfate, filtered, and concentrated in vacuo. The crude material was purified by silica gel gradient chromatography (0-75% ethyl acetate in hexanes), providing the titled compound as an off-white foam. HRMS m/z (M+H) 407.2069 found, 407.2078 required.

The synthetic route of 1001401-62-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; LIVERTON, Nigel, J.; SKUDLAREK, Jason, W.; WO2014/176142; (2014); A1;,
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 1001401-62-2 as follows. name: 2-(2H-1,2,3-Triazol-2-yl)benzoic acid

A solution of (3R, 6i?)-6-methylpiperidin-3-ol (5.31 g, 46.1 mmol), 2-(2H-l,2,3- triazol-2-yl)benzoic acid (10.5 g, 55.3 mmol), EDC (17.7 g, 92.0 mmol), l-hydroxy-7- azabenzotriazole (12.6 g, 92.0 mmol), and triethylamine (19.3 mL, 138 mmol) in DMF (300 mL) was stirred at 50 C overnight, then diluted with saturated aqueous sodium bicarbonate and extracted 3x with ethyl acetate. The organics were washed with brine, dried over magnesium sulfate, filtered, and concentrated. The crude material was purified by silica gel gradient chromatography (0-100% ethyl acetate in hexanes), providing the titled compound as a pale yellow solid. LRMS m z (Mu+Eta) 287.3 found, 287.1 required.

According to the analysis of related databases, 1001401-62-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; SKUDLAREK, Jason, W.; WO2015/95442; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 1001401-62-2, The chemical industry reduces the impact on the environment during synthesis 1001401-62-2, name is 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.

General procedure: TBTU (1.1 mmol) was added to a solution of the required carboxylic acid A-1 (1.0 mmol) and DIPEA (2.0 mmol) in DMF (2.0 mL). After stirring at rt for 10 min a solution of the required amine B-3 (1 .0 mmol) in DMF (1.0 mL) was added. The resulting rxn mixture was stirred at rt for up to 3 d before being purified directly by prep. HPLC (method G) to furnish the desired product.

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, 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; ACTELION PHARMACEUTICALS LTD; BOLLI, Martin; BOSS, Christoph; BROTSCHI, Christine; GUDE, Markus; HEIDMANN, Bibia; SIFFERLEN, Thierry; WILLIAMS, Jodi T.; WO2014/57435; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Some common heterocyclic compound, 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, molecular formula is C9H7N3O2, 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. Formula: C9H7N3O2

2- (2H-1,2,3-triazol-2-yl) benzoic acid (0.37 g, 1.96 mmol)Was added to a 100 mL single-necked round bottom flask,Was dissolved in 20 mL of anhydrous dichloromethane, and then thionyl chloride (6 mL, 82.7 mmol) was added slowly,Pyridine (0.04 mL, 0.50 mmol) and gradually warmed to reflux for 3 hours.Stop the reaction, cool, and slowly evaporate the solvent, the product directly into the next step.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1001401-62-2, its application will become more common.

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jin Chuanfei; Wei Dehuo; Xue Yaping; Zhang Yingjun; (44 pag.)CN106674207; (2017); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics