Electric Literature of 1480-65-5 ,Some common heterocyclic compound, 1480-65-5, molecular formula is C5H3ClFN, 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 5-chloro-2-fluoropyridine (500 mg, 3.80 mmol), DIEA (1.5 g, 11.61 mmol), methyl 2-(piperidin-4-yl)acetate (599 mg, 3.81 mmol) in DMSO (10 mL) was stirred for 16 h at 90 ¡ãC under N2. The resulting solution was extracted with 2×50 mL of EtOAc, and the combined organic layers were concentrated under vacuum and purified with silica gel chromatography using EtOAc / hexane (1/1) to afford 700 mg (69percent) of the title compound as an off-white solid. -MS (ES, m/z): 268.9
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,1480-65-5, its application will become more common.
Reference:
Patent; CENTAURUS THERAPEUTICS; ROMERO, Donna L.; MCCALL, John M.; BLITZER, Jeremy; (118 pag.)WO2018/112077; (2018); A1;,
Pyridine – Wikipedia,
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