Tag: M.W:100-200

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. COA of Formula: C3H3N3O2

1,2,3-Triazole-4-carboxylic acid (45.2 mg, 400 mumol), DIPEA (209 muL, 1.2 mmol) and HCTU (165 mg, 400 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 (S)-2-methoxycarbonylamino-3-methyl-butyryloxymethyl ester (200 mg, 400 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 (15 mg; purity 95%). MS m/z [M+H]+ calc’d for C30H37N5O8, 596.26. found 596.4.

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

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

Related Products of 4314-22-1,Some common heterocyclic compound, 4314-22-1, name is 2-(1H-1,2,3-Triazol-1-yl)acetic acid, molecular formula is C4H5N3O2, 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.

Oxalyl chloride (0.95 ML, 11 mmol) was added dropwise to a suspension of 2- (1- 1, 2,3-triazolyl)) acetic acid (Step B, 1.27 g, 10 mmol) in 10 mL CH2CI2 containing 0.05 mL DMF. Vigorous effervescence was observed. This mixture was stirred at room temperature for 4 h and cooled TO-78C. A solution of N. O- DIMETHYLHYDROXYLAMINE hydrochloride (1.2 g, 13 mmol) and diisopropylethyl amine (6.0 ML, 35 mmol) in 10 mL CH2C12 was added slowly over 3 min. The mixture was then allowed to warm to room temperature and stirred overnight. The reaction mixture was then diluted with ether until no additional precipitate appeared. The solid was filtered and washed with ether. The filtrate was concentrated and the residue was purified on silica gel using EtOAc as solvent to provide the title compound as amorphous solid. 1H NMR (400 MHz, CDC13) : 8 3.252 (s, 3H0, 3.812 (s, 3H), 5.379 (s, 2H), 7.753 & 7.761 (s’s, 2H).

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

Reference:
Patent; MERCK & CO., INC.; WO2004/48317; (2004); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 4928-88-5, 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. 4928-88-5 name is Methyl 1H-1,2,4-triazole-3-carboxylate, 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.

1-(1-Ethoxyethyl)-1,2,4-triazole-3-carboxamide and 1-(1-Ethoxyethyl)-1,2,4-triazole-5-carboxamide. A mixture of methyl 1,2,4-triazole-3-carboxylate (25.4 g, 0.20 mole), dimethylformamide (200 ml), bis(p-nitrophenyl) phosphate (0.20 g), and ethyl vinyl ether (80 ml) was stirred in a stoppered flask at 25¡ã for 120 hrs. The solvent was removed in vacuo and ethyl acetate (300 ml) was added to the residue. A small amount of insoluble material was removed by filtration and the filtrate was evaporated to a syrup. The crude product was treated at 25¡ã for 24 hours with methanol saturated with anhydrous ammonia (300 ml). The solvent was removed in vacuo and addition of ethanol (100 ml) to the residue gave a crystalline product (12.0 g). Recrystallization from ethanol provided 10.0 g (27percent) of pure 1-(1-ethoxyethyl)-1,2,4-triazole-3-carboxamide with mp 163¡ã-166¡ã. Nmr (dmso-d6) delta1.11 (t, 3, J=7Hz, CH3 –CH2 –), 1.70 (d, 3, J=6 Hz, CH3), 3.44 (m, 2, CH3 CH2 –) 5.80 (q, 1, J=6 Hz, C–H), 7.65 and 7.85 (2 S, 2, NH2) 8.90 (s, 1, H-5). Anal. Calcd for C7 H12 N4 O2: C, 45.64; H, 6.57; N, 30.42. Found: C, 45.48; H, 6.61; N, 30.54.

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Methyl 1H-1,2,4-triazole-3-carboxylate, and friends who are interested can also refer to it.

Reference:
Patent; ICN Pharmaceuticals, Inc.; US3991078; (1976); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 15988-11-1, 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 15988-11-1 as follows.

General procedure: General procedure for the synthesis oftriazolo[1,2-a]indazole-trione (1a-g) and2H-indazolo[2,1-b]phthalazine-triones (2a-g)To a well-ground mixture of arylaldehyde (1 mmol), dimedone(0.140 g, 1 mmol) and 4-phenylurazole (0.177 g, 1 mmol) or2,3-dihydrophthalazine-1,4-dione (0.162 g, 1 mmol), was added[Et3N-SO3H]HSO4[(0.028 g, 0.1 mmol) for the preparation of1a-gor (0.042 g, 0.15 mmol] for the synthesis of2a-g}. Theobtained mixture was firstly stirred magnetically at 90C, andafter solidification of the reaction mixture, it was stirred with asmall rod at same temperature. After the reaction was completed(as observed by TLC), the reaction mixture was cooled to roomtemperature, water (2 mL) was added, stirred for 3 min, andfiltered. The solid residue was recrystallized from EtOH/H2O(4/1) to give the pure product.

According to the analysis of related databases, 15988-11-1, the application of this compound in the production field has become more and more popular.

Reference:
Article; Zare, Abdolkarim; Masihpour, Fatemeh; Phosphorus, Sulfur and Silicon and the Related Elements; vol. 191; 8; (2016); p. 1160 – 1165;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 6523-49-5, These common heterocyclic compound, 6523-49-5, name is 4-(1,2,4-Triazol-1-yl)aniline, 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 N’-(3-Cyano-4′-hydroxy-3′-methoxy-biphenyl-4-yl)-N,N-dimethyl- formamidine (220mg) and triazolyl aniline (113mg) in acetic acid (2ml) was heated to 125 for 2h. The cooled mixture was diluted with water and filtered under suction overnight. The resulting solid was sonicated in acetone (20ml) with warming and filtered. The solid was dried to give the title compound as a yellow solid (28mg)..1H NMR (D6-DMSO) delta 3.86 (3H, s); 6.88 (IH, d); 7.28 (IH, d); 7.36 (IH, s); 7.82 (3H, m); 8.03 (2H, m); 8.15 (2H, m); 8.56 (IH, s); 8.69 (IH, s); 9.2 (2H, s); 9.98 (IH, s); LC- MS rt 2.14 m/z 411 ES+

Statistics shows that 4-(1,2,4-Triazol-1-yl)aniline is playing an increasingly important role. we look forward to future research findings about 6523-49-5.

Reference:
Patent; ARROW THERAPEUTICS LIMITED; WO2007/80401; (2007); 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. 252742-72-6, name is 3-(Chloromethyl)-1H-1,2,4-triazol-5(4H)-one belongs to Triazoles compound, it is a common compound, a new synthetic route is introduced below. Safety of 3-(Chloromethyl)-1H-1,2,4-triazol-5(4H)-one

Step 2I-8 2.34200 mg 5-Chloromethyl-2,4-dihydro-[1 ,2,4]triazol-3-one was placed in 25 mL of a 7N solution of ammonia in methanol at ambient temperature. The reaction was stirred overnight and then concentrated under reduced pressure. The product was used without further purification. Yield: 171 mg (100percent of theory)

The synthetic route of 252742-72-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HOFFMANN, Matthias; DAHMANN, Georg; FIEGEN, Dennis; HANDSCHUH, Sandra; KLICIC, Jasna; LINZ, Guenter; SCHAENZLE, Gerhard; SCHNAPP, Andreas; EAST, Stephen P.; MAZANETZ, Michael Philip; SCOTT, John; WALKER, Edward; WO2011/92128; (2011); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route 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.

10.9 mg (0.077 mmol) of 1,2,4-triazole-3-carboxylic acid was dissolved in 5 ml of dichloromethane and 45.2 mg(0.119 mmol) of 2- (7-azobenzotriazole-Nu, Nu, N ‘, N’-tetramethyluronium hexafluorophosphate under ice bath was added 21.9 mg(0.216 mmol) of triethylamine,Stirring for 30min,30 mg of intermediate 121 (0.054 mmol) was added,Stir overnight at room temperature. TLC checkMeasurement,After the reaction,Add lml of saturated sodium bicarbonate solution,Stirring for 20min,Dispensing,The aqueous phase was extracted with dichloromethane,mergeThe organic phase,dry,Steamed in crude.The crude product was purified by preparative silica gel plate (methanol: dichloromethane = 1: 10)The target compound was 9 mg in 21%

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

Adding a certain compound to certain chemical reactions, such as: 135242-93-2, name is (1-Methyl-1H-[1,2,4]triazol-3-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 135242-93-2, HPLC of Formula: C4H7N3O

To a mixture of 176 (1-methyl-1H-1,2,4-triazol-3-yl)methanol (400 mg, 3.54 mmol) and 177 iodobenzene diacetate (1.25 g, 3.89 mmol) in 68 dichloromethane (10 mL) was added 178 TEMPO ((2,2,6,6-tetramethylpiperidin-1-yl)oxyl) (56 mg, 354 mumol). The mixture was stirred at 15-20 C. for 2 h. The mixture was concentrated in vacuo. The residue was purified by silica gel chromatography (petroleum ether:ethyl acetate=1:2) to give 179 1-methyl-1H-1,2,4-triazole-3-carbaldehyde (300 mg, 2.70 mmol, 76% yield). 1H NMR (chloroform-d 400 MHz) delta 10.01 (s, 1H), 8.19 (s, 1H), 4.06 (s, 3H

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it.

Reference:
Patent; H. Lundbeck A/S; Juhl, Karsten; Jessing, Mikkel; Langgard, Morten; Vital, Paulo Jorge Vieira; Kehler, Jan; Rasmussen, Lars Kyhn; Clementson, Carl Martin Sebastian; Marigo, Mauro; (154 pag.)US2019/194189; (2019); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 59660-30-9, 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. 59660-30-9 name is (4-Methyl-4H-[1,2,4]triazol-3-yl)methanol, 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 (4-methyl-l,2,4-triazol-3-yl)methanol (45.83 mg, 0.41 mmol), 5-[4- (trifluoromethoxy)phenyl]-3H-oxazolo[4,5-b]pyridin-2-one (60 mg, 0.20 mmol), PPI13 (106.26 mg, 0.41 mmol) and DIAD (81.92 mg, 0.41 mmol) in THF (3 mL) was stirred at 20 C under N2 for 16 hours. The reaction was diluted with sat.NH4Cl (10 mL), and the mixture was extracted with EtOAc (10 mL x 2). Then the combined organic phase was washed with brine (10 mL), dried over Na2SC>4, filtered and concentrated to give the crude product. The crude product was purified by Prep-HP LC (Waters Xbridge (150 mm x 25 mm, 5 muiotaeta) A = H20 (10 mM NH4HCO3) and B = CH3CN; 32 – 47% B over 8 minutes) to give the impure product. The impure product was triturated from z-Pr20 (10 mL) and purified by Prep-HP LC (Waters Xbridge (150 mm x 25 mm, 5 muiotatauiota) A = H20 (10 mM NH4HCO3) and B = CH3CN; 33 – 63% B over 6 minutes) to give the product (16.59 mg, 41.1 muiotatauiotaomicron, 20% yield) as a solid. 1H NMR (DMSO-c 400MHz) deltaH = 8.48 (s, 1H), 8.14 (d, 2H), 7.88 (d, 1H), 7.81 (d, 1H), 7.48 (d, 2H), 5.30 (s, 2H), 3.79 (s, 3H). LCMS Rt = 1.10 min in 2.0 min chromatography, MS ESI calcd. for CnHnFjNsOs [M+H]+ 392.1, found 391.9.

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

Reference:
Patent; PRAXIS PRECISION MEDICINES , INC.; REDDY, Kiran; MARTINEZ BOTELLA, Gabriel; GRIFFIN, Andrew, Mark; MARRON, Brian, Edward; (244 pag.)WO2018/148745; (2018); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

4928-88-5, name is Methyl 1H-1,2,4-triazole-3-carboxylate, 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. Application In Synthesis of Methyl 1H-1,2,4-triazole-3-carboxylate

EXAMPLE 3 A mixture of methyl 1,2,4-triazole-3-carboxylate (26.4 g, 0.21 mole) and beta-D-ribofuranosyl-1,2,3,5-tetraacetate (60.2 g, 0.19 mole) was melted and then 1.1 g of p-toluenesulfonic acid was added thereto. The reaction mixture was reacted for 3 hours, while maintaining the temperature of the reaction mixture at 105+-5¡ã C. And then, the reaction mixture was crystallized with 300.8 ml of methanol to give 58.6 g of 1-(2,3,5-tri-O-acetyl-beta-D-ribofuranosyl)-1,2,4-triazole-3-carboxylic acid methyl ester (yield: 80percent).

The synthetic route of 4928-88-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Lee, Tai-Au; Park, Nam-Jin; Khoo, Ja-Heouk; Lee, Byung-Cheol; US2003/120064; (2003); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics