Category: 4928-87-4

4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, 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. Product Details of 4928-87-4

A mixture of 3-(6-phenylpyridin-3-yl)-5-(piperidin-4-yl)-8,9- dihydropyrazolo[l,5-a]pyrido[3,2-e]pyrimidin-6(7H)-one (70 mg, 0.17 mmoL), 1H- 1,2,4- triazole-3-carboxylic acid (20.5 mg, 0.18 mmoL), EDC (63 mg, 0.33mmoL), HOBt (44.6 mg, 0.33 mmoL) and DIEA (172.2 uL, 0.99 mmoL) in DMF (3 mL) was stirred at room temperature for 2h. Purification with prep-LC provided 5-(l-(4H-l ,2,4-triazole-3- carbonyl)piperidin-4-yl)-3~(6-phenylpyridin-3-yl)-8,9-dihydropyrazolo[l,5-a]pyrido[3s2- e]pyrimidin-6(7H)-one: LCMS tR = 3.15 Min (10 rain run, UV 254nm)- Mass calculated for, M+ 519.2, observed LC/MS m/z 519.97 (M+H).

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

Reference:
Patent; SCHERING CORPORATION; MENG, Zhaoyang; REDDY, Panduranga Adulla, P.; SIDDIQUI, M. Arshad; MANDAL, Amit, K.; LIU, Duan; ZHAO, Lianyun; MCRINER, Andrew; WO2012/27234; (2012); 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. 4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, A new synthetic method of this compound is introduced below., SDS of cas: 4928-87-4

To a reaction of 1/7-1, 2, 4-triazole-3 -carboxylic acid (100 mg, 0.87 mmol) and 4- Methoxy-3- (trifluoromethyl)benzylamine (200 mg, 0.97 mmol) in dry DMF (10 mL) was added 1- hydroxybenzotriazole monohydrate (146 mg, 0.97 mmol) and EDC (N-(3- Dimethylaminopropyl)-N’-ethylcarbodiimide) (186 mg, 0.97 mmol) followed by N- methylmorpholine (0.38 mL, 3.48 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 24.0 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, filtered and concentrated under reduced pressure and chromatographed on silica gel using EtOAc as eluents to get the desired amide 10 (62.8 mg, 24 % yield) as a white solid compound. -NMR (400 MHz, DMSO-de): <514.66 (br s, 1H), 9.23 (br s, 1H), 8.49 (br s, 1H), 7.60-7.58 (m, 2H), 7.22 (d, J= 8.4 Hz, 1H), 4.43 (d, J= 6 Hz, 2H), 3.86 (s, 3H); 19F -NMR (376 MHz, DMSO-de): <5 -60.82 ppm. MH+ = 301.4 m/z. The synthetic route of 4928-87-4 has been constantly updated, and we look forward to future research findings. 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

Application of 4928-87-4,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.

Example 1: N-[2-[[4-[(lR,3S)-3-[[( lR)-l-(4-Fluoro-3-methoxy-phenyl) ethyl]-amino]cyclopentyl]benzoyl]amino]ethyl]-lH-l,2,4-triazole-3- carboxamide (Compound 101)To a solution of Intermediate 4 (719 mg, 1.8 mmol) in dry DMF (12 mL) was added HOBt (276 mg, 2 mmol) and EDAC (517 mg, 2.7 mmol), and the mixture was stirred at rt for 4 hours. lH-l,2,4-triazole-3-carboxylic acid (200 mg, 1.8 mmol) was then added, and stirring was continued overnight at rt. The solvent was removed under reduced pressure and the crude purified by flash chromatography (30% MeOH/DCM), affording the title compound in 78% yield. *H NMR (300 MHz, DMSO) delta 8.70 (br m, IH), 8.48 (br m, IH), 8.41 (s, IH), 7.76 (d, J = 8.2 Hz, 2H), 7.31 (d, J = 8.2 Hz, 2H), 7.17 (dd, J = 8.6, 1.6 Hz, IH), 7.10 (dd, J = 11.5, 8.3 Hz, IH), 6.89 (ddd, J = 8.1, 4.4, 1.8 Hz, IH), 3.84 (s, 3H), 3.78 (q, J = 6.6 Hz, IH), 3.46 (br m, 4H), 3.04 – 2.85 (m, 2H), 2.15 – 1.54 (m, 6H), 1.43 – 1.19 (m, 4H).

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

Reference:
Patent; LEO PHARMA A/S; MANSSON, Kristoffer; WO2012/69421; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference 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.

Single crystals of 1 were prepared by a branched tube method [13], 1H-1,2,4-triazole-3-carboxylic acid (0.117 g, 1 mmol), lead(II) nitrate (0.331 g, 1 mmol) and potassium bromide (0.119 g, 1 mmol) were placed in the bottom main of a branched tube. Water was carefully added to fill both arms, and then the arm to be heated was placed in oil bath at 60 C. After 3 days, colorless crystals were deposited in the cooler arm which were filtered off, washed with water and air dried. (0.225 g, yield 54%), m.p. ?195 C. (Found C 8.55, H 0.99, N 10.43%. calculated for C3H4BrN3O3Pb; C 8.63, H 0.96, N 10.07%). IR (cm-1) selected bands: 464 (s), 651 (s), 1100 (s), 1303 (m), 1370 (m), 1457 (vs), 1606 (s) and 3370 (br).

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

Reference:
Article; Safarifard, Vahid; Morsali, Ali; Joo, Sang Woo; Ultrasonics Sonochemistry; vol. 20; 5; (2013); p. 1254 – 1260;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Adding a certain compound to certain chemical reactions, such as: 4928-87-4, name is 1,2,4-Triazole-3-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 4928-87-4, COA of Formula: C3H3N3O2

To a reaction of H-, 2, 4-triazole-3 -carboxylic acid (226 mg, 2.0 mmol) and 4- (tert-butyl)aniline (0.33 mL, 2.1 mmol) in dry DMF (10 mL) was added 1- hydroxybenzotriazole monohydrate (337 mg, 2.2 mmol) and EDC (N-(3- Dimethylaminopropyl)-N’-ethylcarbodiimide) (422 mg, 2.2 mmol) followed by N- methylmorpholine (0.88 mL, 8.0 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 24.0 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, filtered and concentrated under reduced pressure and chromatographed on silica gel using EtOAc and Hexanes (60:40) as eluents to get the desired amide 13 (123 mg, 25 % yield) as a white solid compound. -NMR (400 MHz, DMSO-de): (br s, 1H), 7.74 (d, J= 8.8 Hz, 2H), 7.37 (d, J= 8.4 Hz, 2H), 1.28 (s, 9H) ppm. MH+ = 245.2 m/z.

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, 1,2,4-Triazole-3-carboxylic acid, other downstream synthetic routes, hurry up and to see.

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. 4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, A new synthetic method of this compound is introduced below., Application In Synthesis of 1,2,4-Triazole-3-carboxylic acid

To a reaction of 1/7-1, 2, 4-triazole-3 -carboxylic acid (226 mg, 2.0 mmol) and 3,5- dichloroaniline (340 mg, 2.1 mmol) in dry DMF (10 mL) was added 1- hydroxybenzotriazole monohydrate (337 mg, 2.2 mmol) and EDC (N-(3- Dimethylaminopropyl)-N’-ethylcarbodiimide) (422 mg, 2.2 mmol) followed by N- methylmorpholine (0.88 mL, 8.0 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 24.0 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, filtered and concentrated under reduced pressure and chromatographed on silica gel using EtOAc and Hexanes (60:40) as eluents to get the desired amide 14 (68.6 mg, 13 % yield) as a white solid compound. -NMR (400 MHz, DMSO-de): <514.85 (br s, 1H), 10.88 (br s, 1H), 8.69 (br s, 1H), 8.04-7.98 (m, 2H), 7.35-7.33 (m, 1H) ppm. MH+ = 257.3 m/z. 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; 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

Related Products of 4928-87-4, These common heterocyclic compound, 4928-87-4, name is 1,2,4-Triazole-3-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.

A solution of intermediate 27b (0.26 g, 0.58 mmol) in 15 ml of DMF was added EDCI (0.17 g, 0.89 mmol)(0 ¡¤ 12g, 0 ¡¤ 89mmo 1) After stirring and dissolving, 1H-1,2,4-triazole-3-carboxylic acid (0.55 g, 0.44 mmo 1)DIEA 0.2ml (1.17mmol), stirring at room temperature for 12h, TLC detection, the end of the reaction, the liquid spinning was crude, crude by silica gel GColumn chromatography [eluent (methanol: dichloromethane) = 50: 500 (nu: nu)] to give 0.1 g of the title compound of Example 34,Yield: 30.3%

Statistics shows that 1,2,4-Triazole-3-carboxylic acid is playing an increasingly important role. we look forward to future research findings about 4928-87-4.

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

Application of 4928-87-4,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.

Step 5: Preparation of 1-(5-((1 R,3s,5S)-8-(4H-1 ,2,4-triazole-3-carbonyl)-8- azabicyclo[3.2.1]octan-3-yl)-7-amino-3-(6-(1 -methyl-1 H-pyrazol-3-yl)pyridin- yl)pyrazolo[1 ,5-a]pyrimidin-6-yl)ethanone 1 H-1 ,2,4-triazole-3-carboxylic acid (58.0 mg, 0.51 mmol), EDC (133.7 mg, 0.70 mmol), HOBt (94.5 mg, 0.70 mmol) and DIEA (730 uL, 4.20 mmol) were added to a mixture of 1-(7-amino-5-((1 R,3s,5S)-8-azabicyclo[3.2.1]octan-3-yl)-3-(6-(1- methyl-1 H-pyrazol-3-yl)pyridin-3-yl)pyrazolo[1 ,5-a]pyrimidin-6-yl)ethanone (207.7 mg, 0.47 mmol) in DMF (5 mL) and the mixture was stirred at room temperature for 1 h. Purification with prep-LC provided 1-(5-((1 R,3s,5S)-8-(4H-1 ,2,4-triazole-3- carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)-7-amino-3-(6-(1 -methyl-1 H-pyrazol-3- yl)pyridin-3-yl)pyrazolo[1 ,5-a]pyrimidin-6-yl)ethanone.

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

Reference:
Patent; MERCK SHARP & DOHME CORP.; SCHERING CORPORATION; SIDDIQUI, M. Arshad; NAN, Yang; PATEL, Mehul, F.; REDDY, Panduranga Adulla P.; MANSOOR, Umar Faruk; MENG, Zhaoyang; VITHARANA, Lalanthi Dilrukshi; ZHAO, Lianyun; MANDAL, Amit, K.; LIU, Duan; TANG, Shuyi; MCRINER, Andrew; BELANGER, David, B.; CURRAN, Patrick, J.; DAI, Chaoyang; ANGELES, Angie, R.; YANG, Liping; DANIELS, Matthew Hersh; WO2011/90935; (2011); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 4928-87-4,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.

To a reaction of 1/7-1, 2, 4-triazole-3 -carboxylic acid (226 mg, 2.0 mmol) and 4- (trifluoromethyl)aniline (0.28 mL, 2.2 mmol) in dry DMF (10 mL) was added 1- hydroxybenzotriazole monohydrate (337 mg, 2.2 mmol) and EDC (N-(3-Dimethylaminopropyl)-N’-ethylcarbodiimide) (422 mg, 2.2 mmol) followed by N- methylmorpholine (0.88 mL, 8.0 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 24.0 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 EtOAc and Hexanes (80:20) as eluents to get the desired amide 11 (44.4 mg, 9 % yield) as a white solid compound. -NMR (400 MHz, DMSO-de): <514.86 (br s, 1H), 10.90 (br s, 1H), 8.70 (br s, 1H), 8.12 (d, J= 8 Hz, 2H), 7.75 (d, J= 8 Hz, 2H); 19F - NMR (376 MHz, DMSO-de): <5 -60.46 ppm. MH+ = 257.0 m/z. The synthetic route of 4928-87-4 has been constantly updated, and we look forward to future research findings. 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

4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, 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. category: Triazoles

A mixture of 50 mg (0.045 mmol) of compound 136 hydrochloride, 18.8 mg (0.166 mmol) of 1 H-1,2,4-triazol-22.4 mg (0.166 mmol)H0Bt and 31.8 mg EDCISuspended in 4mlTwo gas a burning,Add 58.8 mg(0.581 mmol) of triethylamine,Stirred at room temperature overnight,TLC (DCM: Me0H = 10: l)Showing that most of the raw materials did not react,Additional10 mg of 1H-1,2,4-triazole-3-carboxylic acid,47 mg of HATU and 30 mg of triethylamine,Stirred at room temperature overnight,TLC (DCM: Mu0Eta =10: 1) shows most of the raw material reaction finished,Add 15ml saturated sodium bicarbonate solution for 0.5 hours, the organic phase, the water phase(5: 10) dichloromethane methanol mixture (about 10: 1) extraction, and then 2 1 10 ml of dichloromethane extraction, combined organic phase, dryDry, filtered, evaporated to dryness, preparative TLC purification (dichloromethane: methanol = 10: 1)To give the title compound of Example 51,11mg light yellowThe yield was 21.2%.

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

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