The exploration of chemical space for disease targets is of paramount importance. However, the current repertoire of chemically synthesized compounds, numbering around 108, merely scratches the surface in comparison to the theoretical diversity of 1060. Organic chemists are actively engaged in pioneering methodologies to expand this constrained space. Among these innovative approaches, Asymmetric Carbene Transfer (ACT) emerges as a potent strategy for enhancing molecular diversity. This article critically examines the efficacy of ACT in synthesizing pharmaceutically relevant molecules, encompassing natural products and bioactive compounds. We highlight its pivotal role in the synthesis of 25 compounds. By unraveling the diverse applications of ACT, this review illuminates its potential impact on drug discovery. Furthermore, we propose future methodology directions, contributing to the ongoing discourse within the medicinal chemistry community. In summary, this review article navigates the landscape of ACT, showcasing its prowess in expanding chemical space for drug discovery. Through a nuanced exploration of its applications and a forward-looking approach, we contribute to the collective understanding of ACT's potential and chart a course for future advancements in ACT for drug discovery.
Keywords: Carbene * Natural products * Drug discovery * Structure diversity * Asymmetric synthesis.
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