Application of 351003-36-6, These common heterocyclic compound, 351003-36-6, name is 2-Fluoro-5-iodobenzonitrile, 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 stirred solution of terf-butyl frans-4-(4-chlorophenyl)-3- (hydroxymethyl)piperidine-l-carboxylate (2.20 g, 6.75 mmol) in anhydrous N,N- dimethylformamide (100 mL) was added sodium hydride (0.35 g, 8.8 mmol, 60% w/w dispersion in mineral oil) at 0 C. The reaction mixture was stirred at ambient temperature for 30 minutes. 2-Fluoro-5-iodobenzonitrile (1.83 g, 7.40 mmol) was added at 0 C and the reaction mixture was stirred at ambient temperature for 16 h. Saturated ammonium chloride (50 mL) was added, followed by ethyl acetate (200 mL). The organic layer was washed with brine, dried over anhydrous sodium sulfate and filtered. The filtrate was concentrated in vacuo. The residue was purified by column chromatography (5%-50% gradient of ethyl acetate in hexanes) to afford iert-butyl irans-4-(4-chlorophenyl)-3-((2-cyano-4-iodophenoxy)methyl)piperidine-1-carboxylate in 88% yield (3.30 g) as a colorless solid: MS (ES+) m/z 552.8 (M + 1), 554.8 (M + 1).
The synthetic route of 351003-36-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; XENON PHARMACEUTICALS INC.; SUN, Shaoyi; ZENOVA, Alla, Yurevna; CHAFEEV, Mikhail; JIA, Qi; ZHANG, Zaihui; OBALLA, Renata, Marcella; WO2013/64983; (2013); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com