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