CAS: 123948-88-9; (S)-10-((Dimethylamino)Methyl)-4-Ethyl-4-Hydroxy-3,14-Dioxo-3,4,12,14-Tetrahydro-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinolin-9-Yl Acetate
- 英文名称(S)-10-((Dimethylamino)Methyl)-4-Ethyl-4-Hydroxy-3,14-Dioxo-3,4,12,14-Tetrahydro-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinolin-9-Yl Acetate
- 中文名称托泊替康醋酸盐; 醋酸拓扑替康; 4-乙基-4,9-二羟基-10-[(二甲基氨基)甲基]-1H-吡喃并[3',4':6,7]中氮茚并[1,2-b]喹啉-3,14(4H,12H)-二酮醋酸盐
- IUPAC名称(S)-10-((dimethylamino)methyl)-4-ethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl acetate
- 其它别名Topotecanacetate; 4-Ethyl-4,9-Dihydroxy-10-[(Dimethylamino)Methyl]-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinoline-3,14(4H,12H)-Dione Acetate; (S)-10-((Dimethylamino)Methyl)-4-Ethyl-4,9-Dihydroxy-1,12-Dihydro-14H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinoline-3,14(4H)-Dione Acetate; (S)-10-((Dimethylamino)Methyl)-4-Ethyl-4,9-Dihydroxy-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinoline-3,14(4H,12H)-Dione Acetate
- CAS编号123948-88-9
- MFCD编号:MFCD00884565
- 分子式:C25H25N3O6分子量:463.49
- 产品CID: 344272
- 同类组份化合物CAS123948-88-9 (acetate)123948-87-8 (free base)119413-54-6 (HCl)
- 产品分类分析化学 → 标准品 → 药典标准品和杂质标准品
物理性质
MSDS等安全信息
上下游产品
formaldehyd (S)-10-hydroxycamptothecin acetic acid dimethyl amine(S)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-12-methylene-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione (S)-10-hydroxycamptothecin Topotecan hydr°Chloride camptothecin合成工艺路线路线简述
- 合成目标产物 Topotecanacetate 主要起始原料 Formaldehyde And 10-Hydroxycamptothecin And Acetic Acid And Dimethylamine
- (文献来源)合成步骤主要原料 Formaldehyde 和 10-Hydroxycamptothecin 和 Acetic Acid 和 Dimethylamine
📜喜树碱 以 水 用作溶剂,化学反应 42.0H,反应生成托泊替康醋酸盐; 醋酸拓扑替康; 4-乙基-4,9-二羟基-10-[(二甲基氨基)甲基]-1H-吡喃并[3',4':6,7]中氮茚并[1,2-B]喹啉-3,14(4H,12H)-二酮醋酸盐
参考文献:水溶性(氨基烷基)喜树碱类似物的合成:抑制拓扑异构酶i和抗肿瘤活性.
标题:水溶性(氨基烷基)喜树碱类似物的合成:抑制拓扑异构酶i和抗肿瘤活性.
摘要:制备抗肿瘤生物碱喜树碱(1)的水溶性类似物,其中将氨基烷基引入环a或b.大多数类似物是通过将喜树碱氧化为10-羟基喜树碱(2),然后进行曼尼希反应制得n-取代的9-(氨基甲基)-10-羟基喜树碱(4-12)或随后对曼尼希产品4(13,15,17,19,21)进行修饰.其他化合物则通过修饰2的羟基(25,26)或通过全合成(35,42,43)获得.对这些类似物及其一些合成前体进行了拓扑异构酶i抑制,细胞毒性和抗肿瘤活性的评估.尽管这些测定之间没有定量相关性,但抑制拓扑异构酶i的化合物也具有细胞毒性,并在体内具有抗肿瘤活性.对最具活性的水溶性类似物的进一步评估导致选择9-[((二甲基氨基)甲基]-10-羟基喜树碱(4,Sk&f 104864)作为抗肿瘤药物.除了其水溶性,从天然喜树碱合成的简便性和高效力外,4在临床前肿瘤模型中还表现出广谱活性,目前正在癌症患者中进行i期临床试验.
Doi:10.1021/jm00105A017
海关参考信息
- 2902300000-甲苯
2905122000-异丙醇
2905310000-1,2-乙二醇
2905320000-1,2-丙二醇 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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主要参考文献
1: Alshammari MK, Alghazwni MK, Alharbi AS, Alqurashi GG, Kamal M, Alnufaie SR, Alshammari SS, Alshehri BA, Tayeb RH, Bougeis RJM, Aljehani AA, Alotaibi NM, Abida A, Imran M. Nanoplatform for the Delivery of Topotecan in the Cancer Milieu: An Appraisal of its Therapeutic Efficacy. Cancers (Basel). 2022 Dec 22;15(1):65. doi: 10.3390/cancers15010065.
2: Mills H, Acquah R, Tang N, Cheung L, Klenk S, Glassen R, Pirson M, Albert A, Hoang DT, Van TN. A Critical Scrutiny on Liposomal Nanoparticles Drug Carriers as Modelled by Topotecan Encapsulation and Release in Treating Cancer. Evid Based Complement Alternat Med. 2022 Aug 9;2022:7702512. doi: 10.1155/2022/7702512. Retraction in: Evid Based Complement Alternat Med. 2023 Dec 13;2023:9816492. doi: 10.1155/2023/9816492.
3: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Topotecan. 2021 Aug 16. 13(1):39. doi: 10.3390/pharmaceutics13010039.
合成参考文献
合成方法参考DOI号:10.1021/jm00105a017
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