The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.
本发明涉及高对映体纯度的内酰胺取代
丙酸衍
生物及其制造和使用方法。本发明采用多步合成法生产内酰胺化合物。在反应序列的一个步骤中,对一种内酰胺-烯酰胺进行不对称氢化,生成一种最终可转化为一系列药物化合物的中间体。本发明还考虑原位合成多步合成的中间体,这为内酰胺化合物的整体合成提供了经济优势。