| 第 45 卷第 4 期 |  | Vol. 45 No. 4 | | 2015 年 8 月 | Aug 2015 |
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所屬欄目：醫藥及中間體
5-（2-氟苯基）吡咯-3-甲醛的合成工藝研究 |
| 徐 成，周愛(ài)新，關(guān) 東，王桂艷*
（佳木斯大學(xué) 藥學(xué)院，黑龍江 佳木斯 154007） |
| 摘 要：以1H吡咯為原料，經(jīng)三異丙基氯硅烷N-烴化保護后，再與Vilsmeier試劑進(jìn)行反應得3-醛基-1-H吡咯，再經(jīng)N-溴代丁二酰亞胺（NBS）溴化與2-氟苯硼酸進(jìn)行Suzuki偶聯(lián)反應制得5-（2-氟苯基）吡咯-3-甲醛粗品，粗品用甲苯精制�？偸章�35.5%。該合成工藝操作簡(jiǎn)單，條件溫和，試劑價(jià)廉易得，具有工業(yè)化前景。 |
| 關(guān)鍵詞：抗胃酸；沃諾拉贊；Suzuki偶聯(lián)反應 |
| 中圖分類(lèi)號：R975 文獻標識碼：A 文章編號：1009-9212（2015）04-0046-03 |
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| Synthesis of Important Intermediates for Anti-acid Drug Vonoprazan |
| XU Cheng, ZHOU Ai-xing, GUAN Dong, WANG Gui-yan*
(College of Pharmacy, Jiamusi University, Jiamusi 154007, China) |
| Abstract：Vonoprazan important intermediates were prepared in a series of reactions. At first step intermediate 3 was obtained from the reaction of pyrrole with TIPSCl; and then intermediate 3 reacted with Vilsmeier reagents to give intermediate 4; followed by reacted with NBS, intermediate 5 was obtained; Finally, intermediate 5 reacted with 2-fluorophenyl boronic acid by coupling reaction to give the target compound with an overall yield of 35.5%. This process was suitable for industrial production due to the simple procedures, mild reaction conditions and lower cost. |
| Key words：anti-acid drug; vonoprazan; Suzuki coupling reaction |
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作者簡(jiǎn)介：徐 成（1989-），男，重慶人，碩士研究生，研究方向：創(chuàng )新藥物分子設計、合成與構效關(guān)系研究（E-mail：464890862@qq.com）。
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聯(lián) 系 人：王桂艷，副教授，研究方向：有機合成研究（E-mail：374084560@qq.com）。
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收稿日期：2015-01-02
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