Tag: M.W:100-200

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 16681-70-2 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 butyryloxymethyl ester (51 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 (1 mg; purity 95%). MS m/z [M+H]+ calc’d for C27H32N4O6, 509.23. found 509.4.

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

Synthetic Route of 16681-70-2,Some common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, 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.

B. (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(3H-[1,2,3]-triazole-4-carbonyl)-amino]-pentanoic acid (R7=H) 1,2,3-Triazole-4-carboxylic acid (87.3 mg, 772 mumol, 1.5 eq.) was combined with HATU (293 mg, 772 mumol, 1.5 eq.) and DIPEA (179 muL, 2.0 eq.) and stirred for 5 minutes at room temperature in DCM (3 mL) to yield the activated acid. (2S,4S)-5-Biphenyl-4-yl-4-t-butoxycarbonylamino-2-hydroxymethyl-pentanoic acid ethyl ester (220 mg, 514 mumol, 1.0 eq.) was combined with DCM and TFA (1 mL each), and stirred at room temperature for 1 hour. The mixture was evaporated and azeotroped with toluene (2*). The activated acid was added and the resulting mixture was stirred for 2 hours. The reaction was quenched with water and extracted with DCM. The layers were separated, and the organic layer was dried and evaporated. Two-thirds of the product was purified by preparative HPLC to yield compound A (R7=-CH2CH3) (60 mg, 98% purity), MS m/z [M+H]+ calc’d for C23H26N4O4, 423.40. found 423.2. One-third of the product was hydrolyzed by adding 1 M of NaOH in water (619 muL) in THF (1 mL). The mixture was stirred at room temperature for 1 hour. The solvent was evaporated and the resulting material purified by preparative HPLC to yield compound B (R7=H) (35 mg, 99% purity), MS m/z [M+H]+ calc’d for C21H22N4O4, 395.16. found 395.2.

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

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

Reference of 4922-98-9, 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 4922-98-9 as follows.

General procedure: Solution A. A solution of KOH (0.56 g, 0.01 mol) and potassium salt of ethyl nitrocyanoacetate (1.96 g, 0.01 mol) in2 (8 ml) was stirred at room temperature for 3 h, then kept overnight. 4 M aqueous KOAc (8 ml, 0.03 mol) was added to the resulting solution, and the mixture cooled to 5¡ã. A mixture of 3-aminoazole 1a?i (0.010 mol), EtOH (10 ml),H2O (10 ml), and concentrated HCl (2.5 ml, 0.030 mol)was treated with a solution of NaNO2 (0.759 g, 0.011 mol)in H2O (3 ml) at ?5 ¡ã. The reaction mixture was kept at this temperature for 10 min, then added to the solution A. The mixture was kept at room temperature for 1 h; the formed precipitate was filtered, stirred with 40percent aqueous H2SO4 (10 ml) (AcOH (10 ml) was used for compound 4e), filtered, and dried. The obtained hydrazone 3a?i was heated under reflux in DMF for 3 h. The solvent was evaporated, the residue triturated in water, filtered, and dried.

According to the analysis of related databases, 4922-98-9, the application of this compound in the production field has become more and more popular.

Reference:
Article; Voinkov, Egor K.; Ulomskiy, Eugeny N.; Rusinov, Vladimir L.; Chupakhin, Oleg N.; Gorbunov, Evgeny B.; Drokin, Roman A.; Fedotov, Victor V.; Chemistry of Heterocyclic Compounds; vol. 51; 11-12; (2015); p. 1057 – 1060; Khim. Geterotsikl. Soedin.; vol. 51; 11-12; (2015); p. 1057 – 1060,4;,
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 202931-88-2 as follows. name: 1-Methyl-1H-1,2,3-triazole-5-carbaldehyde

Intermediate 9: Step a (4-Chloro-2-methoxy-3-(4-(trifluoromethyl)benzyl)quinolin-6-yl)(1-methyl-1H-1,2,3-triazol-5-yl)methanol To a flask containing 6-bromo-4-chloro-2-methoxy-3-(4-(trifluoromethyl)benzyl)quinoline (1.45 g, 3.37 mmol, Intermediate 5: step d) was added THF (25 mL) and the solution was cooled to -75 C. n-BuLi (2.5 M in hexanes, 1.3 mL, 3.25 mmol) was then added dropwise. After 2 minutes, 1-methyl-1H-1,2,3-triazole-5-carbaldehyde (580 mg, 5.22 mmol, in 3 mL THF) was introduced. The reaction mixture was allowed to warm to -20 C. over 45 minutes at which time the reaction was quenched with aqueous NH4Cl solution. The aqueous portion was extracted with EtOAc (5*40 mL) and the combined organics were washed with brine, dried over MgSO4, filtered and concentrated to dryness. Chromatography on silica gel (5% CH3CN-DCM increasing to 30% CH3CN+2% MeOH) provided the title compound as an off white amorphous solid.

According to the analysis of related databases, 202931-88-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; LEONARD, KRISTI A.; BARBAY, KENT; EDWARDS, JAMES P.; KREUTTER, KEVIN D.; KUMMER, DAVID A.; MAHAROOF, UMAR; NISHIMURA, RACHEL; URBANSKI, MAUD; VENKATESAN, HARIHARAN; WANG, AIHUA; WOLIN, RONALD L.; WOODS, CRAIG R.; FOURIE, ANNE; XUE, XIAOHUA; CUMMINGS, MAXWELL D.; US2015/105369; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Related Products of 7343-33-1,Some common heterocyclic compound, 7343-33-1, name is 5-Bromo-1H-1,2,4-triazole, molecular formula is C2H2BrN3, 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 dry round bottom flask was charged with potassium phosphate (K3PO4, 7.74 g, 36.5 mmol), CuI (0.165 g, 0.868 mmol), and 3-bromo-1H-1,2,4-triazole (2.83 g, 19.10 mmol). The flask was evacuated/backfilled with N2 (3*). DMF (34.7 ml) was added, followed by trans-(1R,2R)-N,N’-bismethyl-1,2-cyclohexane diamine (0.274 ml, 1.736 mmol) and 1-iodo-4-(trifluoromethoxy)benzene (5 g, 17.36 mmol). The solution was heated to 110¡ã C. After 48 h, the reaction mixture was cooled to RT, diluted with EtOAc and filtered through Celite?. The filtrate was washed with water (100 mL) containing 10 mL 1 M HCl. The organics were separated, and the aqueous phase was further extracted with EtOAc (3*). The organics were combined, dried, and concentrated in vacuo. Purification via flash column chromatography (EtOAc/hexanes) yielded the title compound as a tan solid (1.86 g, 34percent): 1H NMR (400 MHz, CDCl3) delta 8.44 (s, 1H), 7.70 (d, J=8.9 Hz, 2H), 7.38 (d, J=8.5 Hz, 2H); 19F NMR (376 MHz, CDCl3) delta -58.04; EIMS m/z 307 ([M]+).

The synthetic route of 7343-33-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Dow AgroSciences LLC; GIAMPIETRO, Natalie C.; DENT, III, William Hunter; US2014/275565; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Some common heterocyclic compound, 4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, molecular formula is C3H3N3O2, 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: 1,2,4-Triazole-3-carboxylic acid

To a reaction of 1/7-1, 2, 4-triazole-3 -carboxylic acid (113 mg, 1.19 mmol) and 4- (trifluoromethoxy)benzylamine (0.20 mL, 1.31 mmol) in dry DMF (10 mL) was added 1- hydroxybenzotriazole monohydrate (200 mg, 1.31 mmol) and EDC (N-(3- Dimethylaminopropyl)-N’- ethylcarbodiimide) (251 mg, 1.31 mmol) followed by N- methylmorpholine (0.52 mL, 4.76 mmol via syringe). The mixture was stirred at room temperature under nitrogen and the solids were gradually dissolved. The contents were stirred at room temperature for 24 h, and then slowly diluted into iced water and extracted with DCM (2 x 50 mL). The DCM phase was washed with ice cold water (2 x 100 mL). The DCM phase was dried over anhydrous Na2S04, concentrated under reduced pressure and chromatographed on silica gel using MeOH and DCM (8:92) as eluents to get the desired amide 8 (305.3 mg, 90 % yield) as a white solid compound. -NMR (400 MHz, DMSO-de): <514.80-14.01 (br s, 1H), 9.25 (br s, 1H), 8.50 (br s, 1H), 7.44 (d, J= 8.4 Hz, 2H), 7.32 (d, J= 8 Hz, 2H), 4.47 (d, J= 6 Hz, 2H); 19F -NMR (376 MHz, DMSO-de): <5 - 56.89 ppm. MH+ = 287.2 m/z. These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4928-87-4, its application will become more common. Reference:
Patent; THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE; NATIONAL JEWISH HEALTH; WEMPE, Michael Fitzpatrick; VAZQUEZ-TORRES, Andres; DAI, Shaodong; (72 pag.)WO2020/41556; (2020); 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. 1142927-05-6, name is 1-Methyl-1H-1,2,4-triazole-3-carbonitrile, A new synthetic method of this compound is introduced below., Recommanded Product: 1-Methyl-1H-1,2,4-triazole-3-carbonitrile

1-methyl-3-cyano-1H-1,2,4-triazole (20 g, 185 mmol) and anhydrous methanol (500 mL) were added to 100 mL of dry three-Followed by the addition of sodium methoxide (14 g, 259 mmol) and amine chloride(14.8 g, 277.5 mmol),Stir at 5 C for 12 hThe filter,The filtrate was evaporated under reduced pressure,The residue was beaten with acetone,filter,A white solid (23.44 g, 78.8%) was obtained.

The synthetic route of 1142927-05-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Zhang Yingjun; Liu Xinchang; Ren Qingyun; Wang Chaolei; S ¡¤geerdeman; (50 pag.)CN103664899; (2017); B;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Some common heterocyclic compound, 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, 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. Quality Control of 1H-[1,2,3]Triazole-4-carboxylic acid

3-Bromo-1-propyne (1a, 23.8 g, 0.200mol) was dissolved in methanol (100 mL), charged with sodium azide (11.8 g, 0.1815 mol) inwater (50 mL), and stirred at room temperature for 14 h. The mixture was added to a solution of sodium hydroxide (36.3 g, 0.908 mol) in methanol (700 mL) and heated under reflux for 2 h. Themethanol was evaporated and the residue diluted with water (400 mL). Potassium hydroxide (17.7g, 0.315 mol) was added to the solution, which was charged in portions with potassium permanganate (41.1 g, 0.259 mol). The mixture was stirred for 12 h at room temperature and,thereafter, heated at 70 C for 3 h. The suspension was filtered and the clear filtrate dissolved in hydrochloric acid. During the evaporation of the volatiles, carboxylic acid 1269 crystallized in thecold solution. The solid was separated by filtration and heated at 300 C in an open apparatus of recondensation to remove carbon dioxide. The triazole 13 (4.18 g, 60.5 mmol, 33%, based onsodium azide) was isolated by recondensation (5¡¤10-3 mbar) at room temperature.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 16681-70-2, its application will become more common.

Reference:
Article; Banert, Klaus; Hagedorn, Manfred; Hemeltjen, Claudia; Ihle, Andreas; Weigand, Kevin; Priebe, Hanno; Arkivoc; vol. 2016; 5; (2016); p. 338 – 361;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

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.

HATU (79 mg, 207 .imol) was added to a stirred solution of 1H-1,2,3-triazole-4- carboxylic acid (23 mg, 207 .imol) in DMF (1.3 mL) and stirred for 10 minutes. DIPEA (49 mg, 376 .imol) was added and after 5 minutes, Compound 2 (66 mg, 188 .imol) pre5 dissolved in DMF and DIPEA (1.3 mL, 2 eq.) was added. After 90 minutes LCMSindicated the major product. The mixture was then concentrated in vacuo. The product was determined to be a mixture of the isomers with an additional impurity. The product was purified by preparative HPLC to yield the title isomer a (2.75 mm retention time; 1.1 mg) and b (2.68 mm retention time; 3.1 mg) as TFA salts.

The synthetic route of 1H-[1,2,3]Triazole-4-carboxylic acid 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.; WO2015/116760; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference 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.

Example 35 3,5-Dichlorobenzyl 4-(2-(N-methyl-1H-1,2,3-triazole-4-carboxamido)ethyl)piperidine-1-carboxylate The title compound was prepared analogously to Example 34, step 3 from 1H-1,2,3-triazole-4-carboxylic acid and 3,5-dichlorobenzyl 4-(2-(methylamino)ethyl)piperidine-1-carboxylate (Example 1, step 3) (200 mg, 0.579 mmol); LCMS: Rt=1.23 mins; MS m/z 440.5 and 442.5 [M+H]+ for Cl isotopes; Method 2minLowpHv01

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

Reference:
Patent; Novartis AG; Legrand, Darren Mark; Furminger, Vikki; Thomson, Christopher; Hughes, Owen Rhys; Stanley, Emily; US2014/171403; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics