METHOD FOR SYNTHESIS OF EPOTHILONE DERIVATIVES, NOVEL EPOTHILONE DERIVATIVES, AS WELL AS NOVEL INTERMEDIATE COMPOUNDS FOR REALISING SAID METHOD AND SYNTHESIS METHODS THEREOF Russian patent published in 2010 - IPC C07D493/04 A61K31/427 A61P35/00 A61K31/335 C07D313/00 C07D417/06 

Abstract RU 2404985 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel epothilone derivatives of formula (8) , to synthesis method thereof and use thereof to obtain compounds of formula (9) , as well as to novel intermediate compounds for realising said method and synthesis methods thereof. The abbreviation P in said general structural formulae denotes a protective group of a functional hydroxyl selected from silyl protective groups, R2 denotes a 5-member heteroaryl containing N and S as heteroatoms, optionally substituted with C1-C6 alkyl, and R1 denotes methyl.

EFFECT: method of obtaining novel epothilone derivatives is simpler and better, can be well implemented on an industrial scale owing to a shorter synthesis path, and provides high reproducibility of synthesis of highly pure key intermediate compounds and end products.

21 cl, 6 ex

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RU 2 404 985 C2

Authors

Kokh Guido

Lauzeler Oliv'E

Dates

2010-11-27Published

2003-09-12Filed