申请人:Merck Sharp & Dohme Corp.
公开号:US20170275300A1
公开(公告)日:2017-09-28
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,包括钯催化偶联反应。本文提供了一种使用钯催化烷基化反应合成头孢菌素化合物的方法,其化学式为(I),以及相关的组合物。在一个方面,本文提供了一种制备化合物(II)或其盐的方法,包括将化合物(III)或其盐与亲核试剂(Nuc)在存在以下试剂的情况下混合,例如反应:(a)钯源; 和(b)钯结合配体,以形成化合物(II)或其盐。