[EN] PREPARATION OF MAYTANSINOID ESTERS<br/>[FR] PRÉPARATION D'ESTERS DE MAYTANSINOÏDE
申请人:BIO THERA SOLUTIONS LTD
公开号:WO2014094354A1
公开(公告)日:2014-06-26
Provided are efficient methods for direct coupling of a maytansinoid with a carboxylic acid to prepare a maytansinoid C-3 ester in high yield using a rare earth metal-based or trifluoromethanesulfonate-based Lewis acid catalyst and a base together with a coupling reagent. Also provided are compositions used in such methods.
提供了一种高效的方法,用稀土金属基或三氟甲磺酸盐基的路易斯酸催化剂和碱以及偶联试剂直接偶联马坦西酮与羧酸,以高收率制备马坦西酮C-3酯。还提供了在这种方法中使用的组合物。