| 第 51 卷第 2 期 |  | Vol. 51 No. 2 | | 2021 年 4 月 | Apr 2021 |
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所屬欄目：醫藥及中間體
醫藥中間體4-［（4-甲基-1-哌嗪基）羰基］苯胺的合成研究 |
| 姜曉曄，張 煥，雷 雪，黎七雄*
（武漢城市學(xué)院，湖北 武漢 430083） |
| 摘 要：以氮甲基哌嗪為原料，經(jīng)對硝基苯甲酰氯�；拖趸鵉e粉還原兩步反應合成了醫藥中間體4-［（4-甲基-1-哌嗪基）羰基］苯胺，并通過(guò)單因素實(shí)驗優(yōu)化合成工藝。�；磻喝軇镃H2Cl2，縛酸劑為K2CO3，收率95.67%。還原反應用NH4Cl活化后的Fe粉為還原劑，投料比為n（4-［（4-甲基-1-哌嗪基）羰基］硝基苯）∶n（鐵粉）∶n（NH4Cl）=1∶4∶4，收率90.14%�？偸章�82.97%。 |
| 關(guān)鍵詞：4-［（4-甲基-1-哌嗪基）羰基］苯胺；醫藥中間體；單因素實(shí)驗 |
| 中圖分類(lèi)號：R97 文獻標識碼：A 文章編號：1009-9212（2021）02-0038-04 |
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| Synthesis of 4-[(4-Methyl-1-piperazinyl)carbonyl] Aniline as a Medicine Intermediate |
| IANG Xiao-ye, ZHANG Huan, LEI Xue, LI Qi-xiong*
(Wuhan City College, Wuhan 430083, China) |
| Abstract：4-[(4-Methyl-1-piperazinyl)carbonyl] aniline was synthesized through a two-step reaction including acylation and reductionby one-factor experiment to determine the most excellent synthesis process using nitrogen-methyl piperazine as the raw material. The results showed that: in acylation reaction, N-methyl piperazine and p-nitrobenzoyl chloride were reacted to prepare 4-[(4-methyl-1-piperazinyl) carbonyl] nitrobenzenethe;a yield of 95.67% was achieved using CH2Cl2 as the solvent and K2CO3 as the deacid reagent.While in thereduction reaction,the reduction4-[(4-Methyl-1-piperazinyl)carbonyl]nitrobenzene by Fe was actived by NH4Cl to preparation 4-[(4-methyl-1-piperazinyl) carbonyl] aniline;a yield of 90.14% was achieved when.the ratio of 4-[(4-methyl-1-piperazinyl) carbonyl] nitrobenzene: iron: NH4Cl was 1∶4∶4. A total yield of 82.97% was achieved. |
| Key words：4-[(4-methyl-1-piperazinyl) carbonyl] aniline; medicine intermediate; one-factor experiment |
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作者簡(jiǎn)介：姜曉曄（1987—），女，湖北武漢人，碩士，研究方向：藥物合成反應（E-mail：511811879@qq.com）。
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聯(lián) 系 人：黎七雄，教授，研究方向：藥學(xué)（E-mail：1015563065@qq.com）。
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收稿日期：2021-04-28
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