PROCESS FOR AN ANTHRACYCLINE DERIVATIVE, AND AN ANTHRACYCLINONE DERIVATIVE USEFUL FOR THE PROCESS

A process for producing an anthracycline derivative represented by the general formula:where R1 is an acyl group, each of X1 and X2 is a hydrogen atom, a methoxy group, a hydroxyl group, a halogen atom or a lower alkyl group, each of Y1 and Y2 is a hydrogen atom, an alkoxy group or a hydroxyl group,...

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Hauptverfasser: ABE, RUMIKO, MATSUMOTO, TERUYO, SUZUKI, MICHIYO, TERASHIMA, SHIRO, KIMURA, YOSHIKAZU
Format: Patent
Sprache:eng
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Zusammenfassung:A process for producing an anthracycline derivative represented by the general formula:where R1 is an acyl group, each of X1 and X2 is a hydrogen atom, a methoxy group, a hydroxyl group, a halogen atom or a lower alkyl group, each of Y1 and Y2 is a hydrogen atom, an alkoxy group or a hydroxyl group, and Z is a hydrogen atom or a protected hydroxyl group, which comprises reacting an anthracyclinone derivative represented by the general formula:where R is a hydrogen atom or a trialkylsilyl group, and X1, X2, Y1, Y2 and Z are as defined above, with a 1-acylsugar derivative represented by the general formula:where R2 is an acyl group and R1 is as defined above, in the presence of a silyl sulfonic acid derivative represented by the general formula:where each of R3, R4 and R5 is an alkyl group and A is an alkyl group, an aryl group, a polyfluoroalkyl group or a hydrogen atom.