CAS: 947687-02-7; (S)-4,8,11-Triethyl-4-Hydroxy-3,14-Dioxo-3,4,12,14-Tetrahydro-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinolin-9-Yl [1,4'-Bipiperidine]-1'-Carboxylate
该化合物是一种半合成衍生物,目的是提高治疗效力和减少不良效应,该化合物与母分子相比,改善了代谢稳定性和药用动力特性,使它成为肿瘤学应用的有希望的候选体.其行动机制包括抑制DNA对甲异构体I的接触,导致DNA损害和癌症细胞迅速分裂中的流行.8点的乙基修改有助于增加脂性,有可能改善组织渗透性和生物利用率.临床初步研究表明,它可以提供一个更广泛的治疗窗口,减少胃肠毒性,同时保持对色切和其他固态的抗扰动.
- 英文名称(S)-4,8,11-Triethyl-4-Hydroxy-3,14-Dioxo-3,4,12,14-Tetrahydro-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinolin-9-Yl [1,4'-Bipiperidine]-1'-Carboxylate
- 中文名称8-乙基伊立替康
- IUPAC名称(S)-4,8,11-triethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl [1,4'-bipiperidine]-1'-carboxylate
- 其它别名[1,4'-Bipiperidine]-1'-Carboxylic Acid (4S)-4,8,11-Triethyl-3,4,12,14-Tetrahydro-4-Hydroxy-3,14-Dioxo-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinolin-9-Yl Ester; 8-Ethyl Irinotecan; Irinotecan Ep Impurity C; Irinotecan Impurity 13; Irinotecan Impurity G; Irinotecan Hydrochloride Impurity C; Irinotecan?11-Ethyl Impurity (Usp); Irinotecan 11-Ethyl Impurity
- CAS编号947687-02-7
- MFCD编号:MFCD29920109
- FDA UNII编号:OG7FYG3IZO
- 分子式:C35H42N4O6分子量:614.73
- 产品CID: 2000088
- 产品分类分析化学 → 标准品 → 药典标准品和杂质标准品
- 相似结构搜索
- InChIKey: IEKWXGPJFJGZSM-DHUJRADRSA-N
- IEKWXGPJFJGZSM-DHUJRADRSA-N
- 计算化学: 氢键受体数8.0氢键供体数1.0可旋转键数6.0
物理性质
MSDS等安全信息
合成工艺路线路线简述
海关参考信息
- 2902600000-乙苯
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
专利信息
专利号:US-9765083-B2
优先权日:2013-12-03
标 题 :Method for the synthesis of irinotecan
发明人：ZABUDKIN ALEXANDER; MATVIENKO VIKTOR
权利人:SYNBIAS PHARMA AG
摘要:The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.
专利号:EP-3030567-B1
优先权日:2013-12-03
标题 :Method for the synthesis of irinotecan
专利号:CA-2924256-C
优先权日:2013-12-03
标 题:Method for the synthesis of irinotecan
专利号:US-2016264590-A1
优先权日:2013-12-03
标题 :Method for the synthesis of irinotecan
专利号:BR-112016012717-A2
优先权日:2013-12-03
标 题 :METHOD FOR THE SYNTHESIS OF IRINOTECAN
专利号:AU-2014359552-B2
优先权日:2013-12-03
标题 :Method for the synthesis of irinotecan
