Abstract

While organic chemistry until the mid-20th century developed primarily around the 'synthesis' of target molecules through total synthesis of complex natural products, from the late 20th century to the present day, efficient and selective synthetic methodologies for individual steps in the synthesis process have emerged as the core of organic chemistry. Herein, we examine the development of modern organic synthesis by analyzing four Nobel Prizes in Chemistry awarded to the field of organic synthesis from 2001 to 2025. These 4 cases converge on three keywords: catalyst, asymmetric, and methodology, demonstrating that the focus of modern organic synthesis has shifted from 'what to make' to 'how to make it.' This signifies an development toward a discipline of precise molecular design characterized by selectivity, efficiency, and sustainability, and through this analysis, we present perspectives on the future direction of organic chemistry.