Category: 4314-22-1

Reference 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.

A mixture of PyBOP (0.08 mmol in 200 mL of DMF), {[3′-(1- piperazinylmethyl)-3-biphenylyl] methyl} amine (44 mmol in 200 mL of DMF) and DIPEA (30 mL) were added to 1 H-1, 2, 3-triazol-1-yl acetic acid (0.07 mmol). The resulting mixture was stirred for 16 hours at room temperature, the solvent was then removed under vacuum. The residue was re-dissolved in methanol and purified by loading onto a SPE cartridge (SCX, 500 mg), washing with MeOH (5 mL), and eluting with a 2M solution of NH3 in MeOH (5 mL). The NH3 fraction was collected and evaporated under vacuum to give a gum which was re-dissolved in 1: 1 CHO3/ TFA (0.5 mL). After stirring for 2 hours, the solvent was removed under vacuum and the residue was purified by MDAP to give the desired compound as a TFA salt. The free base of the compound was obtained by loading the salt onto a SPE cartridge (SCX, 500 mg), washing with MeOH, and eluting with 2M NH3/MeOH. The ammonia fraction was collected and the solvent was removed under vacuum to give the title compound (11.1 mg, 65%). LC/MS: m/z, 391 (M+H), 2. 04 min.

The synthetic route of 4314-22-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; GLAXO GROUP LIMITED; WO2005/87236; (2005); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

4314-22-1, name is 2-(1H-1,2,3-Triazol-1-yl)acetic 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. 4314-22-1

To a stirred mixture of 5 (65 mg, 0.173 mmol), 1 – 1 ,2,3-triazoleacetic acid (6, 22 mg, 0.173 mmol), and Hunig’s base (0.091 mL, 0.522 mmol) in DMF (2 ml) was added HATU (66 mg, 0.174 mmol) and the reaction mixture was stirred for 30 min. The crude mixture was directly purified by prep. HPLC to give 7 (39 mg, 46%). -NMR (400MHz, d6-DMSO): 513.0 (s, IH), 8.34 (bs, IH), 8.16-8.1 1 (m, 2H), 8.00-7.95 (m, 2H), 7.71 (s, IH), 7.55-7.42 (m, 2H), 7.19 (q, IH), 5.51-5.43 (2s, 2H), 4.86-4.83 (m, 2H), 3.81-3.52 (m, 4H), 3.13-3.12 (2s, 3H), 3.04-2.97 (2s, 3H), 2.64-2.63 (2s, 3H). MS (EI) for C24H27N, ,0, found 486 (MH+).

Statistics shows that 4314-22-1 is playing an increasingly important role. we look forward to future research findings about 2-(1H-1,2,3-Triazol-1-yl)acetic acid.

Reference:
Patent; EXELIXIS, INC.; LEAHY, James, William; WO2012/37204; (2012); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

The chemical industry reduces the impact on the environment during synthesis 4314-22-1, name is 2-(1H-1,2,3-Triazol-1-yl)acetic acid, I believe this compound will play a more active role in future production and life. 4314-22-1

Step C N-Methoxy-N-methyl-2-(1-(1, 2, 3-triazolyl)) acetamide 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 CH2C12 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.

The chemical industry reduces the impact on the environment during synthesis 4314-22-1. I believe this compound will play a more active role in future production and life.

Reference:
Patent; MERCK & CO., INC.; WO2005/44785; (2005); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics