GENERAL SYNTHESIS OF MYRIAPORONES Russian patent published in 2008 - IPC C07D303/42 C07D407/06 A61K31/336 

FIELD: chemistry.

SUBSTANCE: invention relates to the compounds with formula , where R, selected from H, SiR'₃, SOR', SO₂R', C(=O)R' or not necessarily substituted C₁-C₆alkyl; R' is selected from the C₁-C₆alkyl group; R" is selected from CH₂OR, C₁-C₆alkyl, C₁-C₆halogenalkyl, C₂-C₆alkenyl or C₁-C₆alkylidene; substitutes are the alkoxigroup. The invention also relates to the compounds with the formula , , , , where R¹, R², R⁴ and R⁶ are selected from PMB, benzyl, 2,6-dimethylbenzyl, o-nitrobenzyl, 2,6-dichlorbenzyl, 3,4-dichlorbenzyl, TBS, TES, TBDPS, TIPS and TMS; R⁵ is selected from OR', N(R')₂, N(R')(C₁-C₄alkoxi); and -R' is selected from C₁-C₆alkyl and C₇-C₁₀aralkyl, L is the stereospecific leaving group. The method for synthesis of the compound with formula 5 is invented, which includes removal of the protective groups from the precursor's hydroxyl groups. The methods for producing the compounds with the formulas 14 and 26 are invented, which include the precursor's tailing by interacting with CH₃C(O)R⁵, where R⁵ is the group selected from OR', N(R')₂, N(R')(C₁-C₄alkoxi); and R' is C₁-C₆alkyl and C₇-C₁₀aralkyl. The method for producing the compounds with the formulas 19 and 30 , which include the precursor's tailing by interacting with ethylmagnesiumbromide. The pharmaceutical composition based on the compound with the formula I with the cytotoxic activity is invented.

EFFECT: production of pharmaceutical agent for tumor treatment is available.

47 cl, 1 tbl, 93 ex