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Chemical Society reviews · 2026

Recent applications of asymmetric hydrogenation in total synthesis of natural products and drugs.

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Li Dong, Lu Jingya, Zhang Yao, Duan Ya-Nan, Zhang Xumu

Аннотация

Natural products with unique structures and promising bioactivities are vital for drug discovery. The efficient and concise synthesis of these natural products and analogues thus becomes even more critical for further drug screening. Over the past several decades, asymmetric hydrogenation has witnessed remarkable progress and evolved into a powerful and versatile strategy for the construction of chiral molecules. Starting from readily available building blocks, the enantioselective asymmetric hydrogenation of unsaturated bonds offers a straightforward strategy for the rapid construction of isolated or contiguous stereogenic centers at both early and late stages. In this review, we present a comprehensive overview of asymmetric hydrogenation of diverse unsaturated bonds, categorized by structural types. In particular, we highlight the application of asymmetric hydrogenation strategies in the total synthesis of natural products and drugs.