[EN] SYNTHESIS OF CEPHALOSPORIN COMPOUNDS<br/>[FR] SYNTHÈSE DE COMPOSÉS DE CÉPHALOSPORINE
申请人:MERCK SHARP & DOHME
公开号:WO2016025839A1
公开(公告)日:2016-02-18
Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof.
本文提供了一种合成头孢菌素抗生素化合物的方法,包括钯催化的偶联反应。本文提供了一种利用钯催化的烷基化反应合成式(I)头孢菌素化合物的方法,以及相关的组合物。在一个方面,本文提供了一种制备式(II)化合物或其盐的方法,包括混合,例如,将式(III)化合物或其盐与核苷(Nuc)在存在以下试剂的情况下进行反应:(a) 钯源;和(b) 钯配体,以形成式(II)化合物或其盐。