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ANTHRACYCLINE GLYCOSIDE* ITS MANUFACTURE AND PHARMACEUTIC COMPOSITION CONTAINING IT AND HAVING ANTICANCER AND ANTILEUKEMIC ACTIVITY

申请公布号:JPS5636498(A)

申请号:JP19800118527

申请日期:1980.08.29

申请公布日期:1981.04.09

申请人:
ERBA CARLO SPA

发明人:ARUBERUTO BARUJIOTSUCHI;JIYUSETSUPE KASHINERI;SERUJIO PENKO;FUEDERIKO ARUKAMONE;OORERIO DEI MARUKO

分类号:C07H5/06;A61K31/70;A61K31/7008;A61K31/7024;A61K31/7028;A61K31/7034;A61K31/704;A61P35/00;A61P35/02;C07H13/08;C07H15/252

主分类号:C07H5/06

摘要:<p>Anthracycline glycosides of the formula I <IMAGE> I wherein R is hydrogen or hydroxy, one of R1 and R2 is methyl and the other of R1 and R2 is hydroxy, and pharmaceutically acceptable acid addition salts thereof, which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with certain novel sugars in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form the corresponding protected glycosides from which the protecting groups are removed. This gives the compounds wherein R is hydrogen. The former are converted to the corresponding hydroxyl compounds by treatment with bromine and sodium formate.</p>

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