Method for the preparation of maytansinoid esters

Details Method for the preparation of maytansinoid esters Method for the preparation of maytansinoid esters

C - Chemistry, Metallurgy

07

D

C07D 491/12 (2006.01) C07D 498/06 (2006.01)

Patent

CA 2601670

Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process of making a maytansinoid ester comprising forming an anion of maytansinol or a maytansinoid bearing a free C- 3 hydroxyl moiety and reacting the anion with an activated carboxyl compound to thereby produce the maytansinoid ester.

La présente invention concerne des processus améliorés de préparation et de purification d'ester de maytansinoïde, en particulier thiol et des maytansinoïdes contenant du disulfure. Dans un aspect de l'invention, ce processus comprend un processus de fabrication d'ester de maytansinoïde qui consiste à former un anion de maytansinol ou un maytansinoïde porteur d'une fraction hydroxyle en C-3 libre et à faire réagir cet anion avec un composé carboxyle activé de façon à produire ainsi cet ester de maytansinoïde.

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