| 摘要 |
<p>PURPOSE: A method for synthesizing 4-demethoxydaunorubicin(idarubicin) is provided to improve the yield of a final product and to ensure quick synthesis cycle. CONSTITUTION: A method for preparing 4-demethoxydaunorubicin or a salt thereof with a structure of chemical formula 1; a step of converting daunorubicin hydrochloride with a structure of chemical formula 2 into 3'-protected daunorubicin(3'-Prot-daunorubicin) with a structure of chemical formula 3 or 4; a step of contacting 3'-Prot-daunorubicin of chemical formula 3 or 4 with soft Lewis acid in an anhydrous solvent to prepare 4-demethyl-3'-Prot-daunorubicin with structures of chemical formulas 5 and 6; a step of contacting 4-demethyl-3'-Prot-daunorubicin with a trifluoromethane sulphonation reagent to prepare 4-O-trifluoromethane sulfonyl-3'-Prot-daunorubicin of chemical formula 7 or 8; a step of contacting the compound with a reducing agent to prepare 4-demethoxy-3'-Prot-daunorubicin of chemical formula 9 or 10; and a step of removing 3'-Prot groups from the compound of chemical formulas 9 or 10.</p> |
