CAS: 86639-52-3; (S)-4,11-Diethyl-4,9-Dihydroxy-1H-Pyrano[3',4':6,7]Indolizino[1,2-B]Quinoline-3,14(4H,12H)-Dione

相似化合物

947687-01-6 78287-26-0 647852-82-2

上下游产品

CAS号78287-27-1 7-乙基喜树碱 | CAS号35364-15-9 氨基酮 | CAS号110351-94-5 (S)-4-乙基-4-羟基-7... | CAS号797762-11-9 7-ethyl-1,2,6,7... | CAS号100286-90-6 盐酸依立替康 | CAS号19685-09-7 (S)-10-羟基喜树碱 | CAS号123-38-6 丙醛 | CAS号102978-40-5 4-乙基-7,8-二氢-4-羟... | CAS号97682-44-5 伊立替康 | CAS号121080-63-5 SN-38葡糖醛酸 | CAS号100286-90-6 盐酸依立替康 | CAS号121098-77-9 SN-38三-O-乙酰基-β-...

7-乙基喜树碱1-氧化物置于硫酸体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 0.5H,以49%的收率获得产物7-乙基-10-羟基喜树碱
参考文献:Synthesis And Antitumor Activity Of 20(S)-Camptothecin Derivatives: Carbamate-Linked,Water-Soluble Derivatives Of 7-Ethyl-10-Hydroxycamptothecin.
标题:Synthesis And Antitumor Activity Of 20(S)-Camptothecin Derivatives: Carbamate-Linked,Water-Soluble Derivatives Of 7-Ethyl-10-Hydroxycamptothecin.
摘要:Nevel 36衍生物(6个)通过单氨基甲酸酯连接,将7-乙基-10-羟基喜树碱(4)的酚羟基与二胺结合,经过合成并在体内评估了它们的抗肿瘤活性.这些衍生物作为盐酸盐在水中有较好的溶解度,且其e内酯环保持完整,并表现出显著的抗肿瘤活性.其中一种衍生物6-27对l1210白血病和其他小鼠肿瘤显示出极佳的活性.其三水合盐酸盐(cpt-11)的结构通过光谱学和结晶学方法得以确定.
DOI:10.1248/cpb.39.1446

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:WO-2024220674-A1
优先权日:2023-04-18
标题:Timescale-guided microfluidic synthesis of polyphenol-iron iii network nanocapsules of hydrophobic drugs
发明人：YEO YOON; HAN BUMSOO; SHEN YINGNAN
权利人:PURDUE RESEARCH FOUNDATION
摘要:A scalable method of continuous microfluidic synthesis of tannic acid-iron III (TA-FeIII) network (TFN) nanocapsules of a hydrophobic drug; a scalable method of continuous microfluidic synthesis of epigallocatechin-3-gallate iron III (EGCG-FeIII) network, (EFN) nanocapsules; hydrophobic drug nanocapsules synthesized in accordance with the method; and a method of administering a hydrophobic drug to a patient in need thereof by administering to the patient the hydrophobic drug nanocapsules.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

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-8722886-B1
优先权日:2012-11-13
标题:Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin
发明人：CHEN XINGHAI; HAUSHEER FREDERICK H; MALAKHOV ANDREY; KOCHAT HARRY
权利人:CHEN XINGHAI; HAUSHEER FREDERICK H; MALAKHOV ANDREY; KOCHAT HARRY; BIONUMERIK PHARMACEUTICALS INC
摘要:The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as