Related Products of 4522-35-4, These common heterocyclic compound, 4522-35-4, name is 3-Iodo-1H-pyrazole, 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.
To a mixture of 3-iodo-liT-pyrazole (407 mg, 2.1 mmol), PdCh(PPh3)2 (82 mg, 0.12 mmol), Cul (22 mg, 0.12 mmol), and Et3N (10 mL) in THF (10 mL) under argon atmosphere was added diethyl 2-(((2f?,3f?,4f?,5f?)-3,4-diacetoxy-5-(6-Ar,/V?-(bis-(/er/-butoxycarbonyl)- amino)-2-chloro-9//-purin-9-yl)-3-ethynyltetrahydrofuran-2-yl) ethoxy)malonate (1 g, 1.2 mmol). The resulting mixture was stirred at 60 C overnight before it was allowed to cool to room temperature and the organic volatile was removed under reduced pressure. The resulting crude residue was purified by flash silica gel column chromatography (60-100% EtOAc in hexanes) to provide diethyl 2-(((2R,3R,4R, 5A>)-3-(( l//-pyrazol-3-yl)ethynyl)-3,4- diacetoxy-5-(6-Af,Ap-(bis-(/c77-butoxycarbonyl)amino)-2-chloro-9//-purin-9-yl)tetrahydro- furan-2-yl)methoxy)malonate as a solid.
The synthetic route of 4522-35-4 has been constantly updated, and we look forward to future research findings.