Tag: M.W:100-200

Application of 16681-70-2, 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. 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.

[0738] To a solution of Compound 1 (9.7 mg, 18 f.tmol) indioxane (180 f.LL) was added HCI (92 f.LL, 368 flillOI). Theresulting solution was stirred at room temperature for 2 hours,and then concentrated in vacuo. In a separate flask, a solutionof 3H-[1,2,3]triazole-4-carboxylic acid (2.5 mg, 22 f.tmol)andHATU (8.4 mg, 22 f.tmol) inDMF (180 f.LL) was stirred atroom temperature for 30 minutes. After this time, a solution ofthe crude amine in DMF (180 f.LL) was added, followed byDIPEA (9.6 f.LL, 55 f.tmol). The resulting solution was stirredfor 1 hour at room temperature then concentrated in vacuowhen the reaction was deemed complete by LCMS to yieldCompound 2 (9.6 mg), which was used without further purification.

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; THERAVANCE BIOPHARMA R&D IP, LLC; Fleury, Melissa; Beausoliel, Anne-Marie; Hughes, Adam D.; Long, Daniel D.; Wilton, Donna A.A.; US2015/210690; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, 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 16681-70-2, Quality Control of 1H-[1,2,3]Triazole-4-carboxylic acid

J. (2S,4R)-5-Biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid butyl ester (R4=H; R7=-(CH2)3CH3) (2S,4R)-4-Amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid (76 mg, 242 mumol) in MeCN (0.4 mL, 8 mmol) and 4 M HCl in 1,4-dioxane (242 muL, 969 mumol) was combined with butan-1-ol (0.5 mL) at 60 C. The resulting mixture was stirred until solid precipitation was observed (~30 minutes). The solvent was evaporated under vacuum and the solids were azeotroped in toluene and dried under vacuum. 1,2,3-Triazole-4-carboxylic acid (0.0274 g, 0.242 mmol), DIPEA (169 muL, 969 mumol) and HATU (92 mg, 242 mumol) were combined in DMF (0.2 mL) and stirred for 5 minutes at room temperature. This was then combined with the dried solids, predissolved in DMF (0.2 mL) and DIPEA (0.5 eq.). The resulting mixture was stirred for 15 minutes and the reaction was quenched with AcOH. The product was purified by preparative HPLC and lyophilized to yield the title compound (30 mg; purity 95%). MS m/z [M+H]+ calc’d for C26H32N4O4, 465.24. found 465.4.

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

Electric Literature of 40253-47-2, 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. 40253-47-2, name is Ethyl 5-methyl-1H-1,2,4-triazole-3-carboxylate belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below.

To a solution of ethyl 5-methyl-lH-l ,2,4-triazole-3-carboxylate (50 mg, 0.28 mmol) and 2-chloro-4-(chloromethyl)pyridine (50 mg, 0.31 mmol) in DMF (2 mL), K2CO3 (116 mg, 0.84mmol) was added. The mixture was stirred at RT overnight, and was then diluted with H20 (20 mL), extracted with EtOAc (3 x 20 mL), 4: 1 CHCl3: PrOH (3 x 20 mL), dried with MgS04 and concentrated under reduced pressure. The crude product was purified on a Biotage pre-packed silica gel column (EtOAc:Hexane 12percent to 100percent EtOAc) to afford ethyl l-((2- chloropyridin-4-yl)methyl)-5-methyl-lH-l ,2,4-triazole-3-carboxylate (29 mg, 40percent) as a white solid. MS(ES+) Ci2H13ClN402 requires: 280 found: 281 [M+H]+.

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, Ethyl 5-methyl-1H-1,2,4-triazole-3-carboxylate, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; JONES, Philip; DIFRANCESCO, Maria, Emilia; PETROCCHI, Alessia; CARROLL, Christopher, L.; MARSZALEK, Joe; CZAKO, Barbara; JOHNSON, Ryan; THEROFF, Jay; WO2014/31936; (2014); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 27996-86-7, name is 4-[1,2,4]Triazol-1-yl-benzaldehyde, 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 27996-86-7, Application In Synthesis of 4-[1,2,4]Triazol-1-yl-benzaldehyde

To a stirred solution of 4-[1,2,4]triazol-1-yl-benzaldehyde (9.0 g, 52 mmol) in 1,4-dioxane (100 mL), were added K2CO3 (10.76 g, 78 mmol) and methyl triphenyl phosphonium bromide (22.2 g, 62.4 mmol) at room temperature. The resultant reaction mixture was heated to 70 C. for 18 h. After completion of the reaction (TLC), the reaction mixture was cooled to room temperature and filtered and the obtained filtrate was concentrated under reduced pressure. Purification by flash chromatography (SiO2, 100-200 mesh; 25-30% EtOAc in petroleum ether) to afforded the title compound as a white solid (5.6 g, 63%): ESIMS m/z 172.09 ([M+H]+).

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-benzaldehyde, and friends who are interested can also refer to it.

Reference:
Patent; Dow AgroSciences LLC; Lo, William C.; Hunter, James E.; Watson, Gerald B.; Patny, Akshay; Iyer, Pravin S.; Boruwa, Joshodeep; US2014/171312; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 16681-70-2, These common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic 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.

To a stirred solution of 500 mg (2.36 mmol) tert-butyl 3,8-diazabicyclo[3.2.1 ]octane-8- carboxylate in 12 mL NMP were added 532 mg 1 H-1 ,2,3-triazole-4-carboxylic acid (4.71 mmol, 2 eq), 1 .23 mL DIPEA (7.07 mmol, 3 eq) and 1 .791 g HATU (4.71 mmol, 2 eq). After stirring overnight at RT, the solution was subjected to preparative HPLC to yield 378 mg (52 %) tert-butyl 3-(1 H-1 ,2,3-triazol-4-ylcarbonyl)-3,8-diazabicyclo[3.2.1 ]octane- 8-carboxylate. (0433) LC-MS (Method 3): Rt = 0.91 min; MS (ESIpos): m/z = 308 [M+H]+ (0434) 1 H-NMR (500 MHz, DMSO-d6) delta [ppm]: 1.43 (9H), 1 .53 – 1 .72 (2H), 1 .83 (2H), 2.92 (1 H), 3.33 (1 H), 4.14 (1 H), 4.21 (1 H), 4.30 (1 H), 4.40 (1 H), 8.29 (1 H), 15.22 (1 H).

The synthetic route of 16681-70-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; KOPPITZ, Marcus; SIEBENEICHER, Holger; STEUBER, Holger; TER LAAK, Antonius; NUBBEMEYER, Reinhard; ROTTMANN, Antje; IRLBACHER, Horst; BADER, Benjamin; PETERS, Michaele; WAGENFELD, Andrea; TEREBESI, Ildiko; (123 pag.)WO2017/202817; (2017); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Some common heterocyclic compound, 27996-86-7, name is 4-[1,2,4]Triazol-1-yl-benzaldehyde, molecular formula is C9H7N3O, 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: C9H7N3O

Weigh 1.73 g (10 mmol) of 1,2,4-triazole benzaldehyde, 4.28 g (10 mmol) of rhodamine hydrazine was dissolved in 20 mL of ethanol, and added to a 100 mL three-necked flask equipped with a thermometer and a stirring apparatus. To the above mixed solution, 0.40 g (7 mmol) of glacial acetic acid was added, and the mixture was refluxed under constant stirring at 80 C for 5 h, cooled to room temperature, and a white solid was precipitated, washed with cold ethanol and dried under vacuum at 50 C for 8 h to obtain a final product compound. (Triazolyl benzaldehyde, rhodamine hydrazine, Schiff base).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 27996-86-7, its application will become more common.

Reference:
Patent; Qilu University of Technology; Duan Hongdong; Zhong Wenxia; Wang Lizhen; (12 pag.)CN109761992; (2019); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 103755-58-4, name is (1-Phenyl-1H-1,2,3-triazol-4-yl)methanol, 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 103755-58-4, name: (1-Phenyl-1H-1,2,3-triazol-4-yl)methanol

Methyl iodide (7.34g, 3.24mL, 51.72mmol, 6equiv.) was added to acetonitrile (10mL) solution of triazole 1 (1.5g, 8.62mmol, 1equiv.) and heated in a teflon lined sealed steel vessel at 80C for 36h. After completion of reaction, solvent was removed under vacuo and washed with ethyl acetate (5¡Á10mL) to give pale yellow crystalline solid in (2.25g) 83% yield. Mp: 140-142C; IR (KBr): 3316 (nuOH), 1597, 1077cm-1; 1H NMR (400MHz, CDCl3) delta: 9.35 (s, 1H), 7.92-7.90 (m, 2H), 7.65-7.63 (m, 3H), 5.15 (d, 2H, J=6Hz), 5.00 (t, 1H, J=6Hz), 4.51 (s, 3H); 13C NMR (100MHz, CDCl3) delta: 145.0, 134.7, 132.2, 130.7, 128.4, 121.7, 53.0 (-CH2-OH), 40.0 (-CH3-N); HRMS (ESI-MS) calcd for C10H13N3O [M+H]+ 191.1059, found 191.1067.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, (1-Phenyl-1H-1,2,3-triazol-4-yl)methanol, and friends who are interested can also refer to it.

Reference:
Short Survey; Saravanakumar, Rajendran; Ramkumar, Venkatachalam; Sankararaman, Sethuraman; Journal of Organometallic Chemistry; vol. 736; (2013); p. 36 – 41;,
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. 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

[0833] lH-1,2,3-triazole-4-carboxylic acid (3.8 mg, 34f.tmol)was combined withHATU (12.9 mg, 34 flillOI) inDMF(2 mL) and stirred at room temperature for 15 minutes. Compound3(60mg, 137 f.tmol)andDIPEA(l6f.LL, 92f.tmol)werethen added. The solution was stirred at room temperature for15 minutes, at which time LCMS showed reaction completion.The solvent was removed in vacuo and the crude residuewas purified by reverse phase chromatography to yield Compoundb (18.5 mg) as a TFA salt. MS m/z [M+Hr calc’d forC26H31CIFN50 4 , 532.21. found 532.

The synthetic route of 16681-70-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; Fleury, Melissa; Beausoliel, Anne-Marie; Hughes, Adam D.; Long, Daniel D.; Wilton, Donna A.A.; US2015/210690; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 13273-53-5, These common heterocyclic compound, 13273-53-5, name is 4-Bromo-1-methyl-1H-1,2,3-triazole, 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 tert-butyl 4-({[2-amino-5-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)pyridin-3-yl]oxy}methyl)piperidine-1 -carboxylate (I-55) (580 mg, 1 .34 mmol), 4-bromo-1 -methyl-1 /-/-1 ,2,3-triazole (260 mg, 1 .61 mmol), Cs2C03 (2 N, 1 .34 mL, 2.68 mmol) in toluene (2 mL) and EtOH (6 mL) was added Pd(PPh3)4 (30.9 mg, 0.0268 mmol). The mixture was thoroughly degassed before heating under nitrogen at 80 C for 18 hr. TLC (EtOAc) indicated the reaction was completed. The mixture was concentrated under vacuum to dryness, and the residue purified by silica gel chromatography (petroleum ether/ EtOAc = 1/1 to 0/1) to give tert-butyl 4-({[2-amino-5-(1 -methyl-1 /-/-1 ,2, 3-triazol-4-yl)pyridin-3-yl]oxy}methyl)piperidine-1 -carboxylate (I-60) (503 mg, 97%) as a white solid.

The synthetic route of 13273-53-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; PFIZER INC.; JOHNSON, Ted William; RICHARDSON, Paul Francis; COLLINS, Michael Raymond; RICHTER, Daniel Tyler; BURKE, Benjamin Joseph; GAJIWALA, Ketan; NINKOVIC, Sacha; LINTON, Maria Angelica; LE, Phuong Thi Quy; HOFFMAN, Jacqui Elizabeth; (335 pag.)WO2016/97918; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 4928-87-4, 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, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

0.15 g (0.31 mmol) of intermediate 20 was dissolved in 30 ml CH2CI2, 0.1 g (0.52 mmol) of EDCI, 0.07 g (0.53 mmol)Eta0BetaTau,After stirring to dissolve, 0.03 g (0.27 mmol)1,2,4-triazole-3-carboxylic acid, stirred at room temperature12h, TLC detection. The reaction was carried out and the crude product was dried and purified by silica gel column chromatography (eluent: methanol / dichloromethane / aqueous ammonia = 50: 500: 1, ¥: ¥ ¥) to give a white solid. Example 16The target product, 0.1 g, yield 55.6%

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; 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