【摘要】 以安非他酮在人体内的活性代谢物羟基安非他酮为先导化合物,利用1-(2-氟苯基)-2-溴-1-丙酮和苯甘氨醇在NMP溶剂中反应,经胺化、环合、酸化合成得到了吗啉环上5位含苯基的新型吗啉醇类化合物.总收率70.3%,新化合物结构经IR1、HNMR、MS确证.该化合物在国内外未见报道.整个合成路线具有反应时间短,条件温和、收率高等优点.更多还原

【Abstract】 3-methyl-5-phenyl-(2-difluorophenyl)-2-morpholinol Hydrochloride was synthesized from 1-(2-difluorophenyl)-2-bromo-1-Acetone and Phenylglycinol in polar solvents NMP by amine,cyclization reaction,reduction and acidification.The yield amounted to 70.3%.The structures of the target compounds were confirmed by means of IR,1H NMR and MS spectra.This new compound has never been reported at home and abroad.The synthesis method in the article has advantages of shortening reaction time,mild conditions and high yield.更多还原