100286-90-6
100286-90-6 結構式
基本信息
伊立替康
鹽酸伊立替康
鹽酸依立替康
CAMPTOTHECIN 11 HYDROCHLORIDE
CAMPTOTHECIN 11 HYDROCHLORIDE,TOPOTECIN
CPT-11
IRINOTECAN HCL
IRINOTECAN HYDROCHLORIDE
(S)-4,11-DIETHYL-3,4,12,14-TETRAHYDRO-4-HYDROXY-3,14-DIOXO-1H-PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLIN-9-YL ESTER
TOPOTECIN HYDROCHLORIDE
(1,4’-bipiperidine)-1’-carboxylicacid,3,4,12,14-tetrahydro-4,11-diethyl-4-hyd
(s)-ydrochlorid
7-ethyl-10-(4-(1-piperidino)-1-piperidino)carbonyloxycamptothecinhydrochlor
campto
roxy-3,4-dioxo-1h-pyrano(3’,4’:6,7)indolizino(1,2-b)quinolin-9-ylester,monoh
topotecin
u10144oe
[1,4Bipiperidine]-1carboxylic acid (S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[346,7]indolizino[1,2-b]quinolin-9-yl ester, Hcl Trihydrate
[1,4'-Bipiperidine]-1'-carboxylic acid, (4S)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester, monohydrochloride (9CI)
[1,4'-Bipiperidine]-1'-carboxylic acid, 4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester, monohydrochloride, (S)-
7-Ethyl-10-[[4-(1-piperidyl)-1-piperidyl]carbonyloxy]camptothecin hydrochloride
Camptothecin 11
物理化學性質
安全數(shù)據(jù)
制備方法
4897-50-1
86639-52-3
100286-90-6
一般步驟：將(S)-4,11-二乙基-4,9-二羥基-1H-吡喃并[3',4':6,7]吲哚嗪并[1,2-b]喹啉-3,14(4H,12H)-二酮（4.5g）和吡啶（60ml）加入反應容器中。在30-40℃下緩慢滴加[1,4'-聯(lián)哌啶基]-1'-碳酰氯鹽酸鹽（3.44g）和三乙胺（4.8ml）溶于75ml二氯甲烷的溶液。維持反應溫度在30-40℃，持續(xù)攪拌1.5小時。隨后加入4-哌啶基哌啶（0.58g），繼續(xù)攪拌0.5小時。通過減壓蒸餾去除二氯甲烷和吡啶，直至反應混合物體積濃縮至約25ml。加入乙腈（100ml），將混合物加熱至60℃并保持一段時間。待混合物冷卻至室溫后，緩慢加入15ml 5％鹽酸水溶液。室溫下攪拌反應混合物約20小時。將混合物冷卻至0±5℃，過濾收集析出的結晶產物，依次用乙腈:水（10:1，10ml）和乙腈（10ml）洗滌。最后，將產物在減壓條件下干燥，得到目標化合物(S)-4,11-二乙基-4-羥基-3,14-二氧代-3,4,12,14-四氫-1H-吡喃并[3',4';6,7]吲哚并[1,2-b]喹啉-9-基[1,4'-聯(lián)哌啶]-1'-羧酸鹽酸鹽6.4克，收率90%。
參考文獻：
[1] Patent: WO2006/84940, 2006, A1. Location in patent: Page/Page column 5-6
常見問題列表
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Topoisomerase I
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Irinotecan hydrochloride is a topoisomerase I inhibitor. Irinotecan inhibits the growth of LoVo and HT-29 cells, with IC 50 s of 15.8 ± 5.1 and 5.17 ± 1.4 μM, respectively, and induces similar amounts of cleavable complexes in both in LoVo and HT-29 cells. Irinotecan suppresses the proliferation of human umbilical vein endothelial cells (HUVEC), with an IC 50 of 1.3 μM.
Irinotecan (CPT-11, 5 mg/kg) significantly inhibits the growth of tumors by intratumoral injection daily for 5 days, on two consecutive weeks in rats, and such effects also occur via continuous intraperitoneal infusion by osmotic minipump into mice. However, Irinotecan (10 mg/kg) shows no effect on the growth of tumor by i.p. Irinotecan (CPT-11, 100-300 mg/kg, i.p.) apparently suppresses tumor growth of HT-29 xenografts in athymic female mice by day 21. The two groups of Irinotecan (125 mg/kg) plus TSP-1 (10 mg/kg per day) or Irinotecan (150 mg/kg) in combination TSP-1 (20 mg/kg per day) are nearly equally effective and inhibit tumor growth 84% and 89%, respectively, and both are more effective than Irinotecan alone at doses of 250 and 300 mg/kg.