CAS: 78287-27-1; (S)-4,11-Diethyl-4-Hydroxy-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinoline-3,14(4H,12H)-Dione

上下游产品

propionaldehyde camptothecin propionic acid Acetic acid 7-[(S)-1-(2-dimethylamino-ethylcarbamoyl)-1-hydroxy-propyl]-12-ethyl-9-oxo-9,11-dihydro-indolizino[1,2-b]quinolin-8-ylmethyl ester Benzoic acid 7-[(S)-1-(2-dimethylamino-ethylcarbamoyl)-1-hydroxy-propyl]-12-ethyl-9-oxo-9,11-dihydro-indolizino[1,2-b]quinolin-8-ylmethyl ester 4-Methoxy-benzoic acid 7-[(S)-1-(2-dimethylamino-ethylcarbamoyl)-1-hydroxy-propyl]-12-ethyl-9-oxo-9,11-dihydro-indolizino[1,2-b]quinolin-8-ylmethyl ester 7-ethyl-10-hydroxycamptothecin irinotecan

7-Ethyl-18,19-Dehydrocamptothecin置于palladium 10% On Activated Carbon 氢气体系中,用 1,4-二氧六环,乙醇 作为反应溶剂,化学反应 7.0H,反应生成 7-乙基喜树碱
参考文献:Ep2011797
标题:Ep2011797

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:US-5633260-A
优先权日:1994-04-19
标 题 :11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof
发明人：HAUSHEER FREDERICK H; HARIDAS KOCHAT
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients. The present invention also claims 11,7-HECPT and 11,7-HMCPT compositions, the synthesis of 11,7-HECPT or 11,7-HMCPT, the methods of formulation of 11,7-HECPT or 11,7 -HMCPT, and the methods of use of 11,7-HECPT or 11,7-HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7-HECPT or 11,7-HMCPT formulations to humans with various forms of cancer. Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.

专利号:US-7151179-B2
优先权日:2003-05-12
标题 :Process for the preparation of 7-alkyl-10-hydroxy-20(S)-camptothecin
发明人：LIN CHIEN-HSING; CHEN YUNG-FA; CHEN KAU-MING
权利人:SCINOPHARM TAIWAN LTD
摘要:The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S)-camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily available 20(S)-camptothecin. Various other tecan compounds may be made by use of corresponding 7-alkyl-10-hydroxy-20(S)-camptothecin intermediates.

专利号:EP-2065387-B1
优先权日:2007-11-29
标题:Quartz glass micro-photoreactors and synthesis of 10-hydroxycamptothecin and 7-alkyl-10-hydroxycamptothecin
发明人：WERNER SILVIA; SELIGER RAIMUND; RAUTER HOLGER DR; WISSMANN FRIEDRICH DR
权利人:HERAEUS GMBH W C
摘要:Preparation of 10-hydroxycamptothecin and 7-alkyl-10-hydroxycamptothecin, comprises providing a continuous liquid stream with a thickness (d) of a solution of camptothecin-N-oxide or 7-alkyl-camptothecin-N-oxide and passing the stream to at least a light source, which emits light parallel to the thickness (d), where (d) is 10-1000 mu m. An independent claim is included for a device for carrying out the process, comprising two-transparent, flat quartz glass plates, which are arranged parallel to each other at a distance of 10-1000 mu m, two walls, which are in the space between the plates bordering two sides, which are opposite to each other, two openings, which lie opposite to each other and which are not bordered by the walls, two light sources, which are arranged perpendicularly to the plates in such a manner that their radiations penetrate through both the plates into the space, where the plates are connected to each other in a material-closed manner.

专利号:WO-2012032531-A1
优先权日:2010-09-06
标 题:Process for the manufacture of irinotecan hydrochloride by total synthesis
发明人：ALLA VENKATA RAMA RAO; RAO RAMAKRISHNA; RAMARAO CHANDRASHEKAR; NANDIPATI RAMADEVI; CHAMLE VINAY AVINASH
权利人:AVRA LAB PVT LTD; ALLA VENKATA RAMA RAO; RAO RAMAKRISHNA; RAMARAO CHANDRASHEKAR; NANDIPATI RAMADEVI; CHAMLE VINAY AVINASH
摘要:Disclosed herein is a highly safe and easily scalable process for the production of 7-Ethyl- 10-hydroxycamptothecin and its conversion to Irinotecan hydrochloride by total synthesis.

专利号:US-2009143588-A1
优先权日:2007-11-29
标题:Quartz glass micro-photoreactor and synthesis of 10-hydroxycamptothecin and 7-alkyl 10-hydroxycamptothecin