| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to a method of obtaining 10-deacetylbaccatine III with purity of over 99%, which does not contain 10-deacetyl-2-debenzoyl-2-pentenoylbaccatine III. The disclosed method includes: a) treating crude 10-deacetylbaccatine III with an activated derivative of trichloroacetic acid; b) carrying out chromatography on silica gel and elution of 7,10-bis-trichloroacetyl-10-deacetylbaccatine III with dichloromethane or a dichloromethane/ethylacetate mixture; and c) treatment of 10-deacetyl-7,10-bis-trichloroacetylbaccatine III with an alkali followed by crystallisation. The invention also relates to production of paclitaxel, which involves production of 10-deacetylbaccatine III using the disclosed method and its subsequent conversion to N-debenzoylpaclitaxel with its subsequent benzoylation. ^ EFFECT: convenient semi-synthesis of anti-tumour agents with a taxane backbone, which enables to avoid laborious methods of removing corresponding 2-debenzoyl-2-pentenoyl analogues. ^ 7 cl, 1 tbl, 3 ex |
