PURPOSE: To prepare a streoisomer having high carcinostatic actions in high content, by reacting an anthracycline compound with 3,4-dihydro-2H-pyran in an inert solvent in the presence of a metal-containing Lewis acid.
CONSTITUTION: An anthracycline compound shown by the formula I (R is H, halogen, or protected OH) or its acid addition salt is reacted with 3,4-dehydro- 2H-pyran in an inert solvent such as DMF, etc. in the presence of a metal-containing Lewis acid (e.g., 4W6mol AlCl3, TiCl4, etc. is based on 1mol compound shown by the formula I ), to give a streoisomer (namely isomer having high antistatic action) showing a large Rf value during detection with silica gel thin layer chromatography by using a system of CHCl3/CH3OH=9/1 among streoisomers derived from C-2 position in tetrahydropyran-2-yl group of an anthracycline compound derivative shown by the formula II.
TAKEUCHI TOMIO
TATSUTA KUNIAKI
TAKAHASHI YOSHIKAZU
