- Crystalline Polymorphs of Topotecan Hydrochloride and Methods for the Preparation Thereof
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The invention relates to two novel crystalline form of Topotecan hydrochloride (Ia) Herein referred to as forms α and β, characterized by high purity and whose preparation is advantageous from the industrial point of view. Form α can be in fact conveniently prepared starting from 10-hydroxy-camptothecin, whereas form β can be prepared starting from form α.
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Page/Page column 3
(2009/08/14)
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- Crystalline polymorphs of topotecan hydrochloride and methods for the preparation thereof
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The invention relates to two novel crystalline form of Topotecan hydrochloride (Ia) Herein referred to as forms α and β, characterized by high purity and whose preparation is advantageous from the industrial point of view. Form α can be in fact conveniently prepared starting from 10-hydroxy-camptothecin, whereas form β can be prepared starting from form α.
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Page/Page column 4-5
(2009/07/10)
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- PROCESS FOR MAKING TOPOTECAN
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A process of making topotecan or a pharmaceutically acceptable salt thereof comprising reacting an iminium salt with 10-hydroxy-camptothecin.
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Page/Page column 7-8
(2008/12/08)
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- Crystalline forms of topotecan hydrochloride and processes for making the same
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Novel crystalline forms of topotecan hydrochloride and processes of making the same are disclosed.
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Page/Page column 3
(2008/12/04)
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- PROCESS FOR PREPARING TOPOTECAN
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A process for preparing topotecan.
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Page/Page column title page; 7
(2008/06/13)
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- NOVEL CRYSTALLINE POLYMORPHIC FORM OF A CAMPTOTHECIN ANALOGUE
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The invention relates to a novel crystalline form of topotecan hydrochloride, and methods of making the same. The characteristic XRPD pattern and FT-IT patterns are shown in FIGS. 1 and 2.
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Page/Page column 3
(2008/06/13)
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- NOVEL CRYSTALLINE FORMS
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The invention relates to a novel crystalline form of topotecan hydrochloride, and methods of making the same. The characteristic XRPD pattern and FT-IT patterns are shown in Figs. 1 and 2.
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Page/Page column 8
(2008/06/13)
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- PROCESS FOR PREPARING TOPOTECAN FROM 10-HYDROXY-4-(S) CAMPTOTHECIN
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The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan {4-(S)-10 (dimethylamino)-methyl-4-ethyl 4, 9 dihydroxyl-H-pyrano [3'4': 6,7] indolizino-[1,2-b]quinoline-3,14 (4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S) camptothecin.
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- Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin
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The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan{4-(S)-10(dimethylamino)-methyl-4-ethyl 4,9 dihydroxyl-H-pyrano[3′4′:6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S)camptothecin.
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Page column 5
(2008/06/13)
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- Novel syntheses of camptothecin alkaloids. Part 2. Concise synthesis of (S)-camptothecins
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A 9-step, convergent total synthesis of (S)-camptothecin alkaloids is described. The intramolecular [4 + 2] cycloaddition of an N-arylimidate with an alkyne is used to prepare the alkaloid ABC ring system. The chiral center is derived utilizing Seebach's chemistry for the diastereoselective Michael addition of a chiral dioxolanone enolate to a methylene malonate acceptor. The total synthesis of non-racemic topotecan is accomplished from (S)-10-hydroxycamptothecin in an additional step.
- Fortunak, Joseph M.D.,Kitteringham, John,Mastrocola, Antonietta R.,Mellinger, Mark,Sisti, Nicolas J.,Wood, Jeffery L.,Zhuang, Zhi-Ping
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p. 5683 - 5686
(2007/10/03)
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