| 摘要 |
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 |
