Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 4928-88-5.
4928-88-5, These common heterocyclic compound, 4928-88-5, name is Methyl 1H-1,2,4-triazole-3-carboxylate, 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 [LH-[1,] 2,4] triazole-3-carboxylic acid methyl ester (3.0 g, 0.23 mol) in [N, N-DIMETHYLFORMAMIDE] (76 mL) at [25 oC] was treated with triphenylmethylchloride (7.2 g, 0.23 mol) and triethylamine (6.41 mL, 0.23 mol). The reaction mixture was stirred at [25 oC] for 4 days and then diluted with ethyl acetate. The mixture was then washed with a dilute aqueous hydrochloric acid solution. At this time, methanol was added to the organic layer. A precipitate formed and was removed by filtration. The organics were further washed with a saturated aqueous sodium chloride solution, dried over magnesium sulfate, filtered, and concentrated in vacuo. The resulting solid was triturated with diethyl ether. The solid was collected by filtration and washed again with diethyl ether to afford 1-trityl-1H-[1, 2,4] triazole-3-carboxylic acid methyl ester as a white solid (2.45 g, 84percent) which was used without further purification.A solution of 2, 2-dimethyl-propionic acid 8- (4-acetylamino-benzyl)-3-butyl-2, 6- dioxo-1, 2,3, 6-tetrahydro-purin-7-ylmethyl ester (104 mg, 0.22 mmol) in acetonitrile (2.0 mL) was treated with [1,] 8-diazabicyclo [5.4. 0] [UNDEC-7-ENE] (0.03 mL, 0.24 mmol) and [2-BROMOMETHYL-1-FLUORO-4-NITRO-BENZENE] (56.6 mg, 0.24 mmol). The resulting solution was heated to [50 oC FOR] 6 h. At this time, another portion of 1,8- diazabicyclo [5. [4 : 0] UNDEC-7-ENE] (0.03 mL, 0.24 mmol) was added. The reaction was stirred at [25 oC] for 18 h. At this time, the reaction was poured into ethyl acetate (200 mL) and was washed with a 1N aqueous hydrochloric acid solution [(1] x 50 mL) and a saturated aqueous sodium chloride solution [(1] x 50 mL). The organics were dried over magnesium sulfate, filtered, and concentrated in vacuo. Flash chromatography (Merck Silica gel 60,230-400 mesh, 1: 1 ethyl acetate/petroleum ether) afforded 2,2- dimethyl-propionic acid 8- (4-acetylamino-benzyl)-3-butyl-1- (2-fluoro-5-nitro-benzyl)- 2, [6-DIOXO-1,] 2,3, 6-tetrahydro-purin-7-ylmethyl ester (45.3 mg, 33percent) as a tan solid
Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 4928-88-5.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; WO2003/106459; (2003); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics