STAT3抑制剂（HO-3867）的合成工艺改进

doi:10.15952/j.cnki.cjsc.1005-1511.2016.02.15304

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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 LiAlH₄as 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.

Key words： HO-3867 one-pot synthesis semi-continuous synthesis drug synthesis process improvement

Received: 31 August 2015

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	Articles by authors
	SU Jin-cai
	WENG Zhi-bing
	ZHOU Guo-chun

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SU Jin-cai,WENG Zhi-bing,ZHOU Guo-chun. Process Improvement on Synthesis of STAT3 Inhibitor(HO-3867)[J]. Chinese Journal of Synthetic Chemistry, 2016, 24(2): 155-159.

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http://www.hchxcioc.com/EN/10.15952/j.cnki.cjsc.1005-1511.2016.02.15304 OR http://www.hchxcioc.com/EN/Y2016/V24/I2/155

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