本文選題：艾瑞昔布 + 非甾體抗炎藥　； 參考：《中國醫(yī)藥工業(yè)雜志》2017年04期

【摘要】：本研究提供了一條經(jīng)濟(jì)、綠色、適合工業(yè)化生產(chǎn)的工藝路線合成1.1類非甾體抗炎鎮(zhèn)痛藥艾瑞昔布(1)。以2-[4-(甲基磺�；�)苯基]環(huán)氧乙烷(2)為起始原料,經(jīng)加成開環(huán)生成N-正丙基-?-羥基-4-甲磺酰基苯乙胺(3);3與4-甲基苯乙酸在縮合劑羰基二咪唑作用下經(jīng)酸胺縮合生成N-正丙基-N-[2-羥基-2-(4-甲磺�；交�)]乙基-4-甲基苯乙酰胺(4),操作簡(jiǎn)便,收率98%;4經(jīng)Jone's試劑氧化后,在碳酸鉀/乙醇/水體系中(替換文獻(xiàn)的叔丁醇鉀/叔丁醇體系)環(huán)合得1,反應(yīng)時(shí)間從8 h縮短至2 h,收率從61%提高至78%,同時(shí)簡(jiǎn)化了后處理,改善了產(chǎn)品外觀�？偸章�38.5%(以2計(jì)),較文獻(xiàn)提高了12%。
[Abstract]:This study provides an economical, green and suitable industrial route for the synthesis of class 1.1 nonsteroidal anti-inflammatory analgesics. Starting with 2- [4-( methyl sulfonyl) phenyl] ethylene oxide 2), Synthesis of N-n-propyl-4-methylsulfonyl phenylethylamine (N- n-propyl-4-methylsulfonyl phenyl)] ethyl-4-methylphenylethylamine via acid-amine condensation with 4-methylphenylacetic acid in the presence of carbonyl diimidazole by adding ring opening to form N- n-propyl -N- [2-hydroxy-2-N-4-methanesulfonyl phenyl] ethyl-4-methylphenyl Acetamide is simple and easy to operate. After oxidation with Jone's reagent, 1 was synthesized by cyclization in potassium carbonate / ethanol / water system. The reaction time was shortened from 8 h to 2 h, the yield was increased from 61% to 78%, and the reprocessing was simplified. Improved product appearance. The total yield was 38.5%, which was 12% higher than that in the literature.
【作者單位】： 江蘇恒瑞醫(yī)藥股份有限公司;
【分類號(hào)】：R971+.1

【參考文獻(xiàn)】

相關(guān)期刊論文 前1條

1 沈龍海;安泳潼;尹蓓s，

本文編號(hào)：1852314