Reference of 31250-99-4, New Advances in Chemical Research in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 31250-99-4, name is 1-Trityl-1H-1,2,4-triazole, molecular formula is C21H17N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
EXAMPLE 6 This Example illustrates the preparation of 1-trityl-3-bromo-1,2,4-triazole. A stirred solution of 1-trityl-1,2,4-triazole (15.55 g, prepared as described in Example 1) and N,N,N’,N’-tetramethylethylenediamine (5.8 g) in dry tetrahydrofuran (500 ml) was cooled to -70 C. under nitrogen and treated dropwise with n-butyllithium (37.5 ml, 1.6M in hexane). The deep-red solution was stirred at -70 C. for twenty minutes, then treated dropwise with a solution of bromine (10.4 g) in dry tetrahydrofuran (10 ml). The now brownish-yellow solution was allowed to warm to -20 C., quenched with 0.1M sodium thiosulphate solution (150 ml), and extracted with dichloromethane (500 ml). The organic layer was washed with water (4*100 ml), dried and evaporated. The residue was chromatographed on silica, using dichloromethane-ether (25:2) as eluant, to give 1-trityl-5-bromo-1,2,4-triazole (7.86 g, m.p. 239-241 C.). NMR (CDCl3):delta7.1-7.3(15H,m), 7.95(1H,s).
I am very proud of our efforts over the past few months and hope to 1-Trityl-1H-1,2,4-triazole help many people in the next few years.
Reference:
Patent; Zeneca Limited; US5393732; (1995); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics