METHOD OF PRODUCING DOCETAXEL Russian patent published in 2014 - IPC C07D305/14 A61K31/337 A61P35/00 

Abstract RU 2510395 C2

FIELD: chemistry.

SUBSTANCE: compound of formula (I) is obtained by carrying out the following steps: reacting 2-(2,4-dimethoxyphenyl)-3-(2-nitrobenzene suphenyl)-4(S)-phenyl-5(R)-oxazolidene carboxylic acid with 10-deacetyl-bis-7,10-trichloroacetyl baccatin III to obtain 10-deacetyl-7,10-bis-trichloroacetyl baccatin(III)-13-yl ether of 2-(2,4-dimethoxyphenyl)-3-(2-nitrophenzol sulphenyl)-4(S)-phenyl-5(R)-oxazolidine carboxylic acid (VII). Trichloroacetyl groups in positions 7 and 10 of the compound of formula (VII) then undergo hydrolysis to obtain 10-deacetylbaccatin(III)-13-yl ether of 2-(2,4-dimethoxyphenyl)-3-(2-nitrobenzene sulphenyl)-4(S)-phenyl-5(R)-oxazolidine carboxylic acid (VIII). At the last step, the compound of formula (VIII) is treated with acid to obtain 10-deacetyl-N-debenzoyl paclitaxel (I).

EFFECT: improved method of producing docetaxel with high degree of purity.

3 cl, 2 dwg, 6 ex

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RU 2 510 395 C2

Authors

Gabetta Bruno

Gambini Andrea

Bombardelli Ehtsio

Fontana Gabriele

Dates

2014-03-27Published

2005-10-07Filed