磷酸哌喹置于磷酸,水体系中,用 甲醇,二氯甲烷 作为反应溶剂,化学反应 2.0H,以99.9%的收率获得产物磷酸哌喹 参考文献: An Improved Process For The Preparation Of Piperaquine[fr] Procédé Amélioré Pour La Préparation De Pipéraquine 标题: An Improved Process For The Preparation Of Piperaquine[fr] Procédé Amélioré Pour La Préparation De Pipéraquine 摘要:本发明涉及一种改进的制备7-氯-4-哌嗪-1-基喹啉(化学式(i))的过程,该化合物是合成哌喋啶或其药用可接受盐的关键中间体.
1: Cahyaningsih U, Sa'diah S, Syafii W, Sari RK, Maring AJ, Nugraha AB. Antimalarial Efficacy of Aqueous Extract of Strychnos ligustrina and Its Combination with Dihydroartemisinin and Piperaquine Phosphate (DHP) against Plasmodium berghei Infection. Korean J Parasitol. 2022 Oct;60(5):339-344. doi: 10.3347/kjp.2022.60.5.339. Epub 2022 Oct 21. 2: Millat-Martínez P, Salman S, Moore BR, Baro B, Page-Sharp M, Batty KT, Robinson LJ, Pomat W, Karunajeewa H, Laman M, Manning L, Mitjà O, Bassat Q. Piperaquine Pharmacokinetic and Pharmacodynamic Profiles in Healthy Volunteers of Papua New Guinea after Administration of Three-Monthly Doses of Dihydroartemisinin-Piperaquine. Antimicrob Agents Chemother. 2022 Aug 16;66(8):e0018522. doi: 10.1128/aac.00185-22. Epub 2022 Jul 6. 3: Amarachi CS, Attama AA, Onunkwo GC. Assessment of the Anti-Malarial Properties of Dihydroartemisinin- Piperaquine Phosphate Solid Lipid-Based Tablets. Recent Adv Antiinfect Drug Discov. 2022;17(2):103-117. doi: 10.2174/2772434417666220606105822. 14(8):2016-2022. doi: 10.14202/vetworld.2021.2016-2022. Epub 2021 Aug 6.
合成参考文献
参考文献:10.1186/1475-2875-10-185|10.1186/1475-2875-10-198 摘要:Menan H, Faye O, Same-Ekobo A, Oga ASS, Faye B, Kiki Barro CP, Kuete T, N'diaye J, Vicky A, Tine R, Yavo W, Kane D, Kassi KF, Kone M. Comparative study of the efficacy and tolerability of dihydroartemisinin - piperaquine - trimethoprim versus artemether - lumefantrine in the treatment of uncomplicated Plasmodium falciparum malaria in Cameroon, Ivory Coast and Senegal. Malaria Journal. 2011 Jul 08;10(1):185. doi: 10.1186/1475-2875-10-185.