Synthesis of β-Lactams by Palladium(0)-Catalyzed C(sp<sup>3</sup>)−H Carbamoylation
作者:David Dailler、Ronan Rocaboy、Olivier Baudoin
DOI:10.1002/anie.201703109
日期:2017.6.12
A general and user‐friendly synthesis of β‐lactams is reported that makes use of Pd0‐catalyzed carbamoylation of C(sp3)−H bonds, and operates under stoichiometric carbon monoxide in a two‐chamber reactor. This reaction is compatible with a range of primary, secondary and activated tertiary C−H bonds, in contrast to previous methods based on C(sp3)−H activation. In addition, the feasibility of an enantioselective
据报道,β-内酰胺的一般且用户友好的合成方法利用了Pd 0催化的C(sp 3)-H键的氨基甲酰化作用,并在化学计量的一氧化碳下在两腔反应器中运行。与以前的基于C(sp 3)-H活化的方法相反,该反应与一系列伯,仲和活化的叔CH键兼容。另外,证明了使用手性亚膦酸酯配体的对映选择性形式的可行性。最后,该方法可用于合成有价值的对映体纯的无β-内酰胺和β-氨基酸。