Application of 1455-77-2,Some common heterocyclic compound, 1455-77-2, name is 3,5-Diamino-1,2,4-triazole, molecular formula is C2H5N5, 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 242-amino-6- [ [4-fluoro-3-(trifluor omethyl)phenyl] methyl] -5-(2-hydroxyethyl)-4H- [1 ,2,4] triazolo [5, 1-b] pyrimidin-7-oneEthyl 2-(4-fluoro-3-(trifluoromethyl)benzyl)-5-hydroxy-3-oxopentanoate (160 mg, 0.48 mmol), lH-l,2,4-triazole-3,5-diamine (71 mg, 0.71 mmol) and 4-methylbenzenesulfonic acid (41 mg, 0.24 mmol) in n-butanol (0.5ml) was heated to 160 ¡ãC in an open vial. The reaction mixture was heated until the reaction mixture melted and became light brown and was then removed from the heat. The crude product was purified with preparative HPLC (Waters X-bridge C18 OBD column, 5mu silica, 30 mm diameter, 150 mm length, using decreasingly polar mixtures of water (containing 0.1percent TFA) and acetonitrile as eluents). Fractions containing pure product was lyophilised to give the title compound (12 mg, 7percent>). 1H NMR (399.99 MHz, DMSO-d6) delta 12.52 (1H, s), 7.64 (1H, m), 7.57 (1H, m), 7.37 (1H, m), 5.99 (2H, s), 4.84 (IH, s), 3.89 (2H, s), 3.62 (2H, t), 2.76 (2H, t). m/z (APCI) (M+H)
The synthetic route of 1455-77-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BENGTSSON, Boel, Ase; BLACKABY, Wesley; CUMMING, John; FAULL, Alan, Wellington; LARSSON, Joakim; NASH, Ian, Alun; OLDHAM, Keith; PAPE, Andrew; WO2011/114148; (2011); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics