Abstract：Methyl 1-oxyl-2,2,5,5-tetramethylpyrroline-3-carboxylate(5a) was prepared by one-pot method of Favorskii reaction and oxidation, using 3,5-dibromo-2,2,6,6-tetramethylpiperidin-4-one as starting material. 3-Hydroxymethyl-1-oxy-2,2,5,5-tetramethyl pyrroline(7) was obtained by low temperature reduction reaction of 5a, using LiAlH4 as reducing agent. HO-3867 was synthesized by semi-continuous method of alkylation reaction of brominized 7 with arylamine. The total yield was 46.3%. The structure was confirmed by 1H NMR and HR-ESI-MS.
苏进财， 翁智兵， 周国春. STAT3抑制剂（HO-3867）的合成工艺改进[J]. 合成化学, 2016, 24(2): 155-159.
SU Jin-cai， WENG Zhi-bing， ZHOU Guo-chun. Process Improvement on Synthesis of STAT3 Inhibitor(HO-3867). Chinese Journal of Synthetic Chemistry, 2016, 24(2): 155-159.