DOCETAXEL POLYMORPHS AND SYNTHESIS METHODS THEREOF Russian patent published in 2011 - IPC C07D305/14 C07D305/00 C07D407/00 C07D493/00 A61K31/337 A61P35/00 

Abstract RU 2437875 C2

FIELD: chemistry.

SUBSTANCE: invention comprises the following steps: a) reaction of a compound of formula V with zinc and acetic acid to obtain a compound of formula VI b) reaction of the compound of formula VI with an acid to obtain a compound of formula VIA and c) reaction of the compound of formula VIA with di-tert-butyldicarbonate to obtain docetaxel. The invention also relates to methods of producing crystalline forms I, II, III, IV, V of docetaxel, crystalline forms I, II, III, IV, V, VI, VII, VIII, IX of docetaxel, methods of producing solid amorphous docetaxel, a method of producing crystalline form I of amorphous docetaxel, as well as a method of producing crystalline form II of docetaxel.

EFFECT: obtaining docetaxel and polymorphs thereof with desired purity and output by using improved synthesis methods, which are simple, environmentally safe, cheap, reliable and well suited for use on an industrial scale.

27 cl, 18 ex, 31 dwg

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RU 2 437 875 C2

Authors

Palle Ragkhaventrachar'Julu Venkata

Narijam Sekkhar Munasvami

Balaraman Selvakumar

Kaliaperumal Neelakandan

Dates

2011-12-27Published

2007-03-20Filed