Bristol-myers Squibb Compnay

Gesellschaft Fuer Biotechnologische Forschung Mbh (gbf)

Gerhard H&ouml;fle

Gregory D Vite

Soong-Hoon Kim

Robert Michael Borzilleri

Thomas Leibold

Michael Sefkow

2,3-olefinic epothilone derivatives

The present invention relates to a process for the preparation of intermediates useful in the synthesis of epothilone analogs by initially enzymatically degrading certain epothilone compounds to form ring-open structures containing a carboxyl group which is esterified, the hydroxyl groups on the moiety protected and the resulting compound oxidized by, e.g. ozone, to form a first intermediate. The first intermediate can be reacted with a triphenylphosphine adduct to yield a compound containing an ester group at position 1 which is subsequently hydrolyzed to form a second intermediate.

Preparation of epothilone intermediates

The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.

12,13-modified epothilone derivatives

12, 13-cyclopropane epothilone derivatives

Epothilones with a modified side chain and process for the preparation thereof are disclosed.

Epothilones with modified side chain

Growing community of inventors

Braunschweig, Germany

Gerhard Höfle

Growing community of inventors

Braunschweig, Germany

Gerhard H&ouml;fle

Gerhard Höfle