Some common heterocyclic compound, 852569-38-1, name is 5-Chloro-4-fluoro-2-iodoaniline, molecular formula is C6H4ClFIN, 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. name: 5-Chloro-4-fluoro-2-iodoaniline
Potassium tert-butoxide (12.52 g, 111.6 mmol) was added at room temperature under nitrogen5-chloro-4-fluoro-2-iodoaniline(5.0, 22.3 mmol) in 250 ml of dry THF. After stirring for 15 minutes, the reaction mixture was added dropwise1- (tetrahydro-2H-pyran-2-yl) -1H-pyrazole-4-carbonyl fluoride(5.67 g, 24.6 mmol) in 30 mL of dry THF. The reaction mixture was addedStirred at room temperature for 4 hours,Then poured into saturated aqueous NaHCO3 and extracted with EtOAc. The organic phase was dissolved with saturated NaClLiquid washing,Dried over Na2SO4 and concentrated to dryness. Purification by flash chromatography on silica gel (cyclohexene / EtOAc: 95/5 to 80/20)To give a red solid which was purified by amine phase flash chromatography (DCM) to give 2.84 g of a white solid (yield: 31%).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 852569-38-1, its application will become more common.
Reference:
Patent; Sanofi; A ·beinazaite; O ·dukeluosi; N ·jiluo; G ·lasali; K ·maikarui; V ·wen; (119 pag.)CN103012397; (2017); B;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com