Abstract
The optically active lactams represent an important structural motif and present in a wide range of natural products, biologically active compounds and drugs. Compared to the synthesis of chiral five‐ and six‐membered lactams, the asymmetric construction of seven‐membered lactams often presents a challenge due to their consequential entropic and enthalpic barriers. Over the past few decades, substantial efforts have been devoted to this field and chemists have developed various efficient strategies for the preparation of seven‐membered lactams. In this review, we will highlight the recent advances in enantioselective formation of seven‐membered lactams and the discussion will be logically divided into three parts according to the reaction mode. The aim of this review is to familiarize the Reader with new synthetic opportunities offered by these interesting methodologies.
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