| 第 51 卷第 5 期 |  | Vol. 51 No. 5 | | 2021 年 10 月 | Oct 2021 |
|
所屬欄目：醫藥及中間體
硫酸氫氯吡格雷有關(guān)物質(zhì)的合成及工藝應用 |
| 劉良輝，李昕穎，胡 昱*
（南昌大學(xué) 化學(xué)學(xué)院，江西 南昌 330036） |
| 摘 要：硫酸氫氯吡格雷是一種通過(guò)抑制血小板聚集高效的抗血栓藥物，臨床上主要用于治療動(dòng)脈粥樣硬化引起的心臟病或中風(fēng)。有關(guān)物質(zhì)的研究是藥品質(zhì)量研究中關(guān)鍵性項目之一，其含量是評價(jià)藥品的純度是否合格的重要指標。結合硫酸氫氯吡格雷成熟合成路線(xiàn)，分析了3個(gè)潛在的硫酸氫氯吡格雷的有關(guān)物質(zhì)，并利用硫酸氫氯吡格雷合成過(guò)程所用到的原料、中間體或成品進(jìn)行了合成制備，通過(guò)1H NMR、13C NMR、HRMS對產(chǎn)物的結構進(jìn)行表征與確證。結合3個(gè)有關(guān)物質(zhì)的監測結果，對硫酸氫氯吡格雷的進(jìn)一步工藝優(yōu)化提出建議。 |
| 關(guān)鍵詞：硫酸氫氯吡格雷；有關(guān)物質(zhì)；合成方法 |
| 中圖分類(lèi)號：TQ463 文獻標識碼：A 文章編號：1009-9212（2021）05-0043-05 |
|
| Synthesis of Related Substances of Clopidogrel Bisulfate and the Innovation of Synthesis Process |
| LIU Liang-hui, LI Xin-ying, HU Yu*
(School of Chemistry, Nanchang University, Nanchang 330036, China) |
| Abstract：Clopidogrel bisulfate is a highly effective antithrombotic drug that inhibits platelet aggregation. It is clinically used to treat heart disease or stroke caused by atherosclerosis. The research of related substances is the key item in the research of drug quality, and it is an important index to evaluate whether the purity of the drug is qualified. Combined with the synthesis route of clopidogrel bisulfate, three potential related substances of clopidogrel bisulfate were analyzed and prepared from the raw materials, intermediates or finished products used in the synthesis process of clopidogrel bisulfate. The structures of three related substances were characterized by 1H NMR, 13C NMR and HRMS. Combined with the monitoring results of three related substances, the process improvement for the synthesis of clopidogrel bisulfate was proposed. |
| Key words：clopidogrel bisulfate; related substances; synthetic methods |
|
作者簡(jiǎn)介：劉良輝（1997—），男，江西贛州人，碩士研究生，研究方向：制藥工藝（E-mail：1638749237@qq.com）。
|
聯(lián) 系 人：胡昱，教授，研究方向：有機功能分子合成和手性藥物制備（E-mail：huyu@ncu.eduicn）。
|
收稿日期：2021-08-03
|
|