METHOD FOR PREPARING TAXANES AND INTERMEDIATE COMPOUND FOR THEIR PREPARING Russian patent published in 2004 - IPC

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for preparing compounds of the formula (I):

wherein R means tert.-butoxycarbonyl, benzoyl or residue of direct or branched aliphatic acid; R₁ means phenyl or direct or branched alkyl or alkenyl; R₂ means hydrogen atom or acetyl. Method involves: a) simultaneous protection of hydroxyl groups at positions 7 and 10 of 10-desacetylbaccatin III with trichloroacetyl derivatives to yield compound of the formula (III):

;

b) the following esterification of hydroxyl group of compound of the formula (III) at position 13 by interaction with compound of the formula (VII):

wherein R means tert.-butoxycarbonyl, benzoyl or residue of direct or branched aliphatic acid; R₁ means phenyl or direct or branched alkyl or alkenyl to yield compound of the formula (IV):

;

c) removal of trichloroacetyl protecting groups in compound of the formula (IV) to yield compound of the formula (V):

;

d) optional selective acetylation of hydroxyl group at position 10 in compound of the formula (V) to yield compound of the formula (VI):

;

e) acidic hydrolysis of oxazolidine ring in compound of the formula (VI) to yield compound of the formula (I). Invention relates also to intermediate compounds of the formula (IV):

wherein R and R₁ have values indicated above.

EFFECT: improved preparing method.

9 cl, 5 ex