SEMISYNTHETIC METHOD AND NEW COMPOUNDS Russian patent published in 2004 - IPC C07D471/18 C07D491/22 C07D515/22 

FIELD: organic chemistry, chemical technology, medicine, oncology.

SUBSTANCE: invention relates to methods for preparing compounds of the formula (XVII b):

wherein R¹ represents optionally protected or modified aminomethylene group, optionally protected or modified hydroxymethylene group; R⁴ represents hydrogen atom (-H); or R¹ and R⁴ form in common group of formulas (IV), (V)

represents hydrogen atom (-H) or -OH; R⁷ represents -OCH₃; R⁸ represents -OH; or R⁷ and R⁸ form in common the group -O-CH₂-O-; R^14a and R^14b represent hydrogen atom (-H), or one represents hydrogen atom (-H) and other represents -OH, -OCH₃ or -ОСН₂-СН₃; or R^14a and R^14b form in common keto-group; R¹⁵ represents hydrogen atom (-H) or -OH; R¹⁸ represents hydrogen atom (-H) or -OH; R²¹ represents hydrogen atom (-H), -OH or CN, and their derivatives. Compounds are synthesized from 21-cyano-compound of the formula (XVIb):

Invention relates also to new compounds of formulas

These compounds elicit both antibacterial and antitumor activity. Invention provides preparing new compounds comprising the condensed system consisting of five rings eliciting valuable pharmacological properties, and in alternative methods for synthesis of some derivatives of ecteinascidine and related compounds. This allows providing more economic ways for preparing antitumor agents and preparing new active compounds.

EFFECT: improved preparing method, valuable medicinal properties of compounds.

52 cl, 4 tbl, 65 ex