ENZYMATIC PROCESS FOR REGIOSELECTIVE MANUFACTURING OF N-Fmoc-DOXORUBICIN-14-O-DICARBOXYLIC ACID MONOESTERS

PROBLEM TO BE SOLVED: To provide a process for regioselective synthesis of N-Fmoc-doxorubicin-14-O-dicarboxylic acid monoester compounds or derivatives thereof.SOLUTION: In a process for synthesis of N-Fmoc-doxorubicin-14-O-dicarboxylic acid monoester compounds represented by the formula (I) or deri...

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Hauptverfasser:	MATTHIAS GERLACH, TILMANN SCHUSTER, FALK SCHUCH
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	BEER BIOCHEMISTRY CHEMISTRY DERIVATIVES THEREOF ENZYMOLOGY FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIREDCHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERSFROM A RACEMIC MIXTURE METALLURGY MICROBIOLOGY MUTATION OR GENETIC ENGINEERING NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY SPIRITS SUGARS VINEGAR WINE
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Beschreibung
Zusammenfassung:	PROBLEM TO BE SOLVED: To provide a process for regioselective synthesis of N-Fmoc-doxorubicin-14-O-dicarboxylic acid monoester compounds or derivatives thereof.SOLUTION: In a process for synthesis of N-Fmoc-doxorubicin-14-O-dicarboxylic acid monoester compounds represented by the formula (I) or derivatives thereof starting from N-Fmoc-doxorubicin using lipase and bis-acyl donor compounds such as dicarboxylic acids or dicarboxylic acid anhydrides, compositions of liquid organic media are examined and acylation is performed at the C14-OH group.SELECTED DRAWING: None 【課題】Ｎ−Ｆｍｏｃ−ドキソルビシン−１４−Ｏ−ジカルボン酸モノエステル化合物又はその誘導体を位置選択的に合成する方法の提供。【解決手段】リパーゼとジカルボン酸又はジカルボン酸無水物の様なビス−アシル供与体化合物を使用し、Ｎ−Ｆｍｏｃ−ドキソルビシンから出発して、式（Ｉ）で表すＮ−Ｆｍｏｃ−ドキソルビシン−１４−Ｏ−ジカルボン酸モノエステル化合物又はその誘導体を合成の際に、液体有機媒体の組成を検討し、Ｃ１４−ＯＨ基においてアシル化する方法。【選択図】なし