Electric Literature of 261762-59-8 ,Some common heterocyclic compound, 261762-59-8, molecular formula is C7H6ClFO, 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 solution of the compound of Reference Example 1 (100 mg, 0.32 mmol) in 1,4-dioxane (0.64 mL) was added (2-chloro-5-fluorophenyl) methanol (120 mg, 0.74 mmol), sodium hydride , 0.80 mmol) at room temperature, and the mixture was stirred at 100 C. for 48 hours. Water (10 mL) was added to the reaction mixture at room temperature and extracted with ethyl acetate (10 mL × 2). The organic layers were combined, dried over sodium sulfate and concentrated. The resulting concentrate was purified by silica gel column chromatography (eluent: ethyl acetate / n-hexane = 30/70) to give an intermediate as a yellow oil (80 mg).To a solution of the obtained intermediate (80 mg) in 1,4-dioxane (0.32 mL) was added 4 N hydrogen chloride 1,4-dioxane solution (0.8 mL) at room temperature, and the mixture was stirred at room temperature for 1 hour. Acetonitrile (5.0 mL) was added to the reaction mixture at room temperature, diethyl ether (1.5 mL) was added dropwise at room temperature, and the mixture was stirred at room temperature for 1 hour. The solid was collected by filtration and dried under reduced pressure at room temperature to give 1- (6 – ((2-chloro-5-fluorobenzyl) oxy) pyrazin-2-yl) -1, 4- diazepane dihydrochloride Compound of Example 8) as a white solid (40 mg, 31% yield).
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 261762-59-8, 2-Chloro-5-fluorobenzyl alcohol, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; TORAY INDUSTRIES INCORPORATED; KIKUCHI, TSUKASA; OKANO, TSUBASA; (24 pag.)JP2017/14121; (2017); A;,
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