78287-27-1
78287-27-1 結(jié)構(gòu)式
基本信息
伊立替康雜質(zhì)16
伊立替康EP雜質(zhì)F
喜樹堿7-乙基雜質(zhì)
伊立替康相關(guān)物質(zhì)E
7-乙基喜樹堿 1G
7-乙基喜樹堿對(duì)照品
伊立替康雜質(zhì)F(EP)
鹽酸伊立替康EP雜質(zhì)F
7-乙基喜樹堿(M1)
(S)-4,11-Diethyl-4-hydroxy-1H-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4H,12H)-dione
(4S)-4,11-Diethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
SN 22
7-Etyl-camptothecin
(4S)-4,11-Diethyl-4-hydroxy-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法
123-38-6
7689-03-4
78287-27-1
向5L反應(yīng)釜中加入80g (S)-4-乙基-4-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（喜樹堿）、840g冰醋酸和368g濃硫酸，啟動(dòng)機(jī)械攪拌至完全溶解。隨后，緩慢加入80g丙醛，并滴加102g過氧化氫?？刂品磻?yīng)溫度在-5至5℃范圍內(nèi)，持續(xù)反應(yīng)10分鐘。反應(yīng)完成后，向體系中加入10kg純水，繼續(xù)攪拌2小時(shí)。通過抽濾收集沉淀，得到72.5g (S)-4,11-二乙基-4-羥基-1H-吡拉諾[3',4':6,7]吲哚并[1,2-b]喹啉-3,14(4H,12H)-二酮（7-乙基喜樹堿），收率為95.4%。
參考文獻(xiàn)：
[1] Patent: CN108484624, 2018, A. Location in patent: Paragraph 0031; 0039; 0043; 0044
[2] Chemical and Pharmaceutical Bulletin, 1991, vol. 39, # 6, p. 1446 - 1454
[3] Chemical and Pharmaceutical Bulletin, 1991, vol. 39, # 10, p. 2574 - 2580
[4] Patent: WO2006/16203, 2006, A1. Location in patent: Page/Page column 9-10
[5] European Journal of Pharmaceutical Sciences, 2018, vol. 123, p. 546 - 559