METHOD OF SYNTHESIS OF CAMPTOTHECIN DERIVATIVES Russian patent published in 2002 - IPC

FIELD: organic chemistry. SUBSTANCE: invention relates to method of synthesis of derivatives of camptothecin of the formula (I) where Y and Z mean hydrogen atom, alkyl, hydroxyalkyl-group or usual protective amino-group; R1 is hydrogen atom, alkyl, hydroxy- group; R2 and R3 are hydrogen atom, hydroxy-group or they can bind to form cyclic methylenedioxy-fragment or ethylenedioxy-group; R4 is hydrogen atom or alkyl; R5 is hydrogen atom, hydroxy-group, fluorine, bromine, chlorine, iodine atom or amino-group. Invention describes the more facility method of synthesis involving synthesis of compound of the formula (I) by Mannich's reaction, i. e. compound of the general formula (II) that reacts with amine or its salt and with formaldehyde source in the presence of acid. EFFECT: improved method of synthesis. 5 cl, 1 sch, 14 ex