The present invention relates to a method comprising the step of contacting under hydroaminomethylation conditions, an olefin, an amine, a rhodium-phosphorous ligand, and synthesis gas (syngas). In particular, it has been discovered that, under some circumstances, a neutral rhodium-monodentate phosphite ligand is prescribed. The invention provides a simple way of making, in high yields and regiospecificity, a variety of products, including pharmacologically active products such as ibutilide, terfenadine, and fexofenadine, and derivatives thereof.
本发明涉及一种方法,其步骤包括在
氢胺甲基化条件下接触烯烃、胺、
铑-
膦配体和合成气(合成气)。特别是,在某些情况下发现,需要使用中性的
铑-单齿
膦酸酯
配体。本发明提供了一种简单的方法,以高产率和区域特异性制备多种产品,包括具有药理活性的产品,如依布利特、特芬那定和费索芬那定及其衍
生物。