Category: 1001401-62-2

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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, A new synthetic method of this compound is introduced below., Safety of 2-(2H-1,2,3-Triazol-2-yl)benzoic acid

General procedure: Et3N (0.45 mL, 3.3 mmol) was added to a solution of 2-(1H-pyrazol-4-yl)ethanamine dihydrochloride (0.30 g, 1.6 mmol) in DMF (5 mL) at room temperature, followed by stirring. 5-Methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid (0.36 g, 1.8 mmol), HOBt.H2O (0.37 g, 2.4 mmol), and EDC.HCl (0.47 g, 2.4 mmol) were added to the reaction solution, followed by stirring at room temperature for 3 hours. An aqueous NaHCO3 solution was added to the reaction mixture, followed by extraction with EtOAc. The organic layer was washed with water and brine and was dried with Na2SO4. The desiccant was then removed by filtration, and the solvent was distilled off under reduced pressure. The resulting residue was purified by column chromatography (KP-NH: 28 g, CHCl3/MeOH=100/0 to 97/3) to give the titled compound (0.43 g, colorless and amorphous). MS (ESI pos.) m/z: 297 [M+H]+

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

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

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

A mixture of 2-(2H-1,2,3-triazol-2-yl)benzoic acid (285 mg, 1.5 mmol) in SOCl2 (3 mL) was stirred at RT for 0.5 h. Then the mixture was concentrated in vacuo. To a solution of the product from step 7 (300 mg, 1.26 mmol) and TEA (0.5 mL, 3.78 mmol) in DCM (3 mL) was added the above residue dropwise at 0 oC. The mixture was stirred at 0 oC for 2 h. water (2 mL) was added to quench the reaction and the mixture was extracted with DCM (3 mL x 3). The combined organic layers was washed with brine (3 mL x 3), dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by Prep-HPLC to give the title compound as a solid. LRMS m/z (M+H) 410.1 found, 410.2 required.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, and friends who are interested can also refer to it.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; LIVERTON, Nigel; LUO, Yunfu; (68 pag.)WO2016/89721; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 1001401-62-2, 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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below.

A solution of 2-(2H-l,2,3-triazol-2-yl)benzoic acid (4.24 g, 22.40 mmol), tert-butyl ((3i?,6i?)-6-methylpiperidin-3-yl)carbamate (3.20 g, 14.93 mmol), l-hydroxy-7-azabenzotriazole (4.06 g, 29.9 mmol), EDC (5.72 g, 29.9 mmol), and DIEA (15.65 mL, 90 mmol) in DMF (100 mL) was heated at 50 C overnight. The reaction was diluted with saturated, aqu. NaHC03 and extracted 2x with EtOAc. The organics were washed with brine, dried over MgS04, filtered, and concentrated. The residue was purified by silica gel gradient chromatography (0-80% EtOAc in hexanes), providing the title compound. LRMS m/z (M+H) 386.4 found, 386.2 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, 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; SKUDLAREK, Jason, W.; WO2015/95441; (2015); 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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, A new synthetic method of this compound is introduced below., SDS of cas: 1001401-62-2

Intermediates 10: N-[(1S,2S)-2-Hydroxycyclopentyl]-2-(2H-1,2,3-triazol-2-yl)benzamide Triethylamine (1.52 ml, 10.90 mmol), 3H-[1,2,3]triazolo[4,5-b]pyridin-3-ol (0.59 g, 4.36 mmol) and EDC (0.84 g, 4.36 mmol) were added to a solution of (1R,2S)-2-aminocyclopentan-1-ol hydrochloride (CAS number 137254-03-6; 0.50 g, 3.63 mmol) and 2-(2H-1,2,3-triazol-2-yl)benzoic acid (CAS number 1001401-62-2; 0.76 g, 4.00 mmol) in DCM (10 ml). The reaction was stirred at room temperature for 18 hours and then diluted with DCM (50 ml) and washed with a saturated solution of sodium bicarbonate (2¡Á20 ml). The crude product was purified by column chromatography (silica, 0-100% ethyl acetate/petrol) to afford the title compound. 1H NMR (400 MHz, DMSO-d6) delta ppm 1.36-1.59 (m, 3H), 1.62-1.88 (m, 3H), 3.79-3.93 (m, 1H), 3.94-4.10 (m, 1H), 4.29-4.39 (m, 1H), 7.49-7.58 (m, 1H), 7.58-7.67 (m, 2H), 7.71-7.82 (m, 2H), 8.05 (s, 2H) MS ES+: 273 Intermediates 11: N-[(1S,2S)-2-Hydroxycyclopentyl]-2-(2H-1,2,3-triazol-2-yl)benzamide Prepared according to the procedure for N-[(1S,2S)-2-hydroxycyclopentyl]-2-(2H-1,2,3-triazol-2-yl)benzamide (Intermediate 10) from 2-(2H-1,2,3-triazol-2-yl)benzoic acid (CAS number 1001401-62-2; 531 mg, 2.81 mmol), (1S,2S)-2-aminocyclopentan-1-ol hydrochloride (CAS number 68327-04-8; 368 mg, 2.67 mmol) and DIPEA (1401 mul, 8.02 mmol) to afford the title compound. 1H NMR (400 MHz, DMSO-d6) delta ppm 1.33-1.48 (m, 2H), 1.49-1.79 (m, 3H), 1.83-1.97 (m, 1H), 3.80-3.88 (m, 1H), 3.89-3.98 (m, 1H), 4.57-4.67 (m, 1H), 7.43-7.55 (m, 2H), 7.56-7.67 (m, 1H), 7.73-7.83 (m, 1H), 8.03 (s, 2H), 8.09-8.23 (m, 1H) MS ES+: 273

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; Takeda Pharmaceutical Company Limited; Fieldhouse, Charlotte; Glen, Angela; Maine, Stephanie; Fujimoto, Tatsuhiko; Robinson, John Stephen; US2015/232460; (2015); 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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below. Recommanded Product: 1001401-62-2

A solution of 2-(2H-1,2,3-triazol-2-yl)benzoic acid (P. Coleman, J. Schreier, WO2007/126934) (1 g, 4.1 mmol) in SOCl2 (10 mL) was stirred at 80 C for 30 min. The solvent was removed under reduced pressure and toluene (10 mL) was added to give solution A. The product from step 4 (1 g, 4.1 mmol) was dissolved in DCM (10 mL), DIEA (1.58 g, 12 mmol) added, and then solution A added at 0 C. The resulting mixture was stirred at RT for 2 h, then poured into water (10 mL) and extracted with DCM (10 mL x 3). The combined organic layers were washed with brine (10 mL), dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by chromatography on silica (petroleum ether : EtOAc = 10 : 1 to = 3 : 1) then purified by prep. TLC (petroleum ether : EtOAc = 1 : 1) to give the title compound (0.2 g). LRMS m/z (Mu+Eta) 416.0, 418.0 found, 416.1, 418.1 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; BESHORE, Douglas, C.; KUDUK, Scott, D.; LUO, Yunfu; MENG, Na; YU, Tingting; WO2015/20930; (2015); 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., Recommanded Product: 2-(2H-1,2,3-Triazol-2-yl)benzoic acid

Step iii) ir 3s-N-{4-[(6-FIuoro-l,3-benzot azol-2-yl)ammo]oxolaii-3-yI}-2-(2H-l,2,3- triazoI-2-y)beiizamide A solution of tran5-3-N-(6-fluoro-l,3-benzothiazol-2-yl)oxolane-3,4-diarriinehydrochloride (106 mg, 0.366 mmol), 2-(2H-l ,2,3-triazol-2-yl)benzoic acid (CAS number 1001401-62-2; 83 mg, 0.439 mmol), EDC (105 mg, 0.549 mmol), aza-HOBt (85 mg, 0.549 mmol ) and triethylamime (0.153 ml, 1 .097 mmol) in DCM (2 ml) was stirred at room temperature for 18 hours. The reaction mixture was diluted with DCM (20 ml) and washed with HC1 (aq., IM, 20 ml) and saturated sodium bicarbonate solution (20 ml). The organics were filtered through a hydrophobic frit and solvent evaporated in vacuo. This was then purified by reverse phase preparative HPLC (acetonitrile / water with 0.1% ammonia) to afford the title compound.1H NMR (400 MHz, CD2C12-d2) : delta ppm 3.58 – 3.95 (m, 2 H), 4.13 – 4.32 (m, 2 H), 4.32 – 4.51 (m, 2 H), 6.77 (br. s., 1 H), 6.96 – 7.11 (m, 1 H), 7.25 – 7.41 (m, 2 H), 7.43 – 7.53 (m, 1 H), 7.56 – 7.65 (m, 2 H), 7.76 (s, 2 H), 7.81 – 7.87 (m, 1 H)MS ES+: 425

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:
Patent; TAKEDA CAMBRIDGE LIMITED; TAKEDA PHARMACEUTICAL COMPANY LIMITED; FIELDHOUSE, Charlotte; GLEN, Angela; ROBINSON, John Stephen; FUJIMOTO, Tatsuhiko; WO2015/55994; (2015); 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. 1001401-62-2, name is 2-(2H-1,2,3-Triazol-2-yl)benzoic acid, A new synthetic method of this compound is introduced below., Safety of 2-(2H-1,2,3-Triazol-2-yl)benzoic acid

A solution of 2-(2H-1,2,3-triazol-2-yl)benzoic acid (227 mg, 1.2 mmol) in 2 mL ofSOC12 was heated at 50 C for 30 mins. After cooling to RT, the mixture was concentrated invacuo. A solution of the product from step 4 (80.0 mg, 0.41 mmol) and TEA (121 mg, 1.2 mmol) in DCM (3 mL) at 0 C was stirred for 10 mm and a solution of the above residue inDCM (1 mL) was added dropwise at 0 C. The mixture was stirred for 40 mins at 0 C. The mixture was concentrated in vacuo. The residue was purified by silica gel columnchromatography (20% EtOAc in petroleum ether) to give the title compound as a solid. LRMS m/z (M+H) 331.2 found, 331.2 required.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; MERCK SHARP & DOHME CORP.; KUDUK, Scott, D.; LIVERTON, Nigel; LUO, Yunfu; (58 pag.)WO2016/89722; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route 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.

To a solution of compound 4 (1.0 g, 4.42 mmol) and 2-(2H-1,2,3-triazol-2- yl)benzoic acid (0.84 g, 4.42 mol) in DCM (50 mL) was added HATU (1.70 g, 4.50 mmol), DIPEA (0.60 g, 4.5 mmol) succesively. The solution was stirred at RT for 9 h under N2, then poured into water (30 mL) and extracted with DCM (20 mL x 3). The combined organic layerswere washed with brine (30 mL), dried over Na2504, filtered and concentrated in vacuo. The residue was purified by column chromatography (petroleum ether: EtOAc = 7: 1 to 2 : 1) to give the title compound 5 (1.5 g,). LRMS m/z (M+H) 398.2 found, 398.2 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.; KIM, Ronald; KUDUK, Scott, D.; LIVERTON, Nigel; ZHUO, Gang; (97 pag.)WO2016/100157; (2016); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route 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: (2-(2H-l,2,3-Triazol-2-yl)phenyl)((2i?,5i?)-5-hydroxy-2-methylpiperidin-l-yl)methanone (6) A solution of (3R, 6i?)-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), 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 title compound as a pale yellow solid. LRMS m/z (Mu+Eta) 287.3 found, 287.1 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.; SKUDLAREK, Jason, W.; WO2014/176144; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics