目的 對脫氫環(huán)氧甲基醌霉素（DHMEQ）的合成工藝進行改進研究。方法 以阿司匹林和2,5-二甲氧基苯胺為起始原料，經(jīng)縮合、碘苯二乙酯氧化、過氧化氫環(huán)氧化、酸催化脫縮酮保護、NaBH₄還原成目標化合物，關(guān)鍵的環(huán)氧化步驟采用HPLC監(jiān)控并通過調(diào)整反應(yīng)條件進行工藝優(yōu)化。結(jié)果 剔除了柱色譜步驟，優(yōu)化后制得的目標化合物質(zhì)量分數(shù)為99.4%，工藝總收率為30.0%。結(jié)論 DHMEQ的合成工藝改進后操作簡便，產(chǎn)品質(zhì)量可控，適合工業(yè)化生產(chǎn)。

Objective To study the improved method for synthesis of dehydroxymethylepoxyquinomicin (DHMEQ). Methods Aspirin and 2,5-dimethoxyaniline were used as starting materials to synthesize the target compound by condensation, oxidation with (diacetoxyiodo)benzene, epoxidation with hydrogen peroxide, deketalization by acid catalysis, and NaBH₄ reduction. The key process was the epoxidation reaction that was monitored by HPLC, and reaction condition was adjusted to optimize the synthetic process. Results The process of column chromatography could be eliminated. After optimization, the purity of target compound was 99.4%, and the total recovery of the synthetic route was 30.0%. Conclusion After optimization, the synthetic process of DHMEQ has the advantage of simple operation, and the product quality can be controlled. Therefore, the improved method for synthesis of DHMEQ is suitable for industrial production of drugs.

國家科技重大專項（2012ZX09103101-004）；廣東省戰(zhàn)略性新興產(chǎn)業(yè)核心技術(shù)攻關(guān)項目（2012A080800010）；深圳市技術(shù)研究開發(fā)計劃（三大產(chǎn)業(yè)）項目（JSA201105090126A）