Abstract: Nitration of 3-fluorophenyl acetic acid (1) was accomplished by heating it to 70 ℃ with nitro-sulfuric acid in dichloroethane for 4 h and 5-fluoro-2-nitrophenyl acetic acid (2) was obtained with 67.8% yield. The obtained compound (2) was treated with borane-tetrahydrofuran (B2H6–THF) complex under nitrogen atmosphere in excessive THF for 18 h to give a kind of dark brown oil，followed by ammonolysis with NH3·H2O in autoclave at 100 ℃ for 6 h to produce 2-(5-amino-2- nitrophenyl) ethanol (3) in 84.4% yield. Catalytic hydrogenation of (3) under 0.6～0.7 MPa. over 10% Pd/C in anhydrous isopropyl alcohol at 70～80 ℃ for 12 h produced 2-(2,5-diamino phenyl)ethanol (4) with 64% yield. Compared with the method reported in literature，the overall yield of target molecule (4) was increased by 11%. The chemical structure of (4) was determined by HPLC-MS and 1H-NMR.

摘要： 在二氯乙烷介质中，将3-氟苯乙酸于70 ℃下硝化4 h得到5-氟-2-硝基苯乙酸（质量分数为67.8％）。用硼烷还原5-氟-2-硝基苯乙酸后，接着用氨水在高压釜中加热到100 ℃氨解，得到2-(5-氨基-2-硝基苯)乙醇（84.4%）。最后，10％Pd/C作催化剂，在无水异丙醇介质中，0.6～0.7 MPa下，于70～80℃催化氢化12 h，得到目标分子2-(2,5-二氨基苯)乙醇（64％）。与文献工艺相比，目标分子总收率提高11％。用H–NMR和MS确定了目标分子2-(2,5-二氨基苯)乙醇的化学结构。