FURO[3,2-B]PYRAN DERIVATIVES, APPLICABLE IN SYNTHESIS OF ANALOGUES Russian patent published in 2016 - IPC C07D493/04 C07D493/18 C07D407/14 C07D407/06 C07D493/22 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formulae

,

or ,

wherein X represents halogen or oxo; Q represents -C(O)H, -CH=CHC(O)OY₁, -C(R)H(CH₂)_nOY₁ or -C(R)HCH₂C(O)OY₁; R represents H; n equals 1 or 2; Y₁, Y₃ and Y₄, each independently represents H or protective group for hydroxyl; T represents oxo or -OY₅; and Y₅ represents H or protective group for hydroxyl or Y₅, together with oxygen atom, which it is bound with, represents leaving group, wherein protective group for hydroxyl Y₁ and Y₅, together with oxygen atom, which each of them is bound with, independently represents C1-C12 alprotective group for hydroxyl, and protective group for hydroxylkyl- or carbocyclic C6-C20 aryl- ester Y₃ and Y₄, together with oxygen atom, which each of them is bound to, independently represents tri(C1-C6alkyl)silyl or- di(C6-C10aryl)(C1-C6alkyl)silyl- ether protective group for hydroxyl, and leaving group represents (C1-C12)alkylsulphonate or carbocyclic (C6-C20)arylsulphonate, which are used to obtain chalichondrin B analogues for synthesis, such as eribulin and its pharmaceutically acceptable salts.

EFFECT: invention also relates to methods for obtaining ER-804028 and eribulin or its pharmaceutically acceptable salt, for instance eribulin mesilate.

28 cl, 2 tbl