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The first, second, and third editions of Catalytic Asymmetric Synthesis published in 1993, 2000, and 2010, respectively, were warmly received by research communities in academia and industries, from graduate students, research associates, faculty, staff, senior researchers, and others. Catalytic Asymmetric Synthesis has become a common tool for the synthesis of enantiopure compounds in both industry and academia.

The Nobel Prize in Chemistry 2001 was given to W. Knowles, K. B. Sharpless, and R. Noyori for their outstanding contributions to the advancement of catalytic asymmetric synthesis, using transition‐metal catalysis. Quite recently it was announced that Benjamin List and David MacMillan won the Nobel Prize in Chemistry 2021 for their work on the development of asymmetric organocatalysis, using small organic molecule. This is the second Nobel Prize given to the field of asymmetric catalysis, following the Nobel Prize in Chemistry 2001, which clearly indicates the profound importance of asymmetric catalysis.

More than 10 years have passed after the third edition was published, and 2010s has witnessed revolutionary advancement of asymmetric catalysis. Therefore, the publication of the fourth edition of this book series, capturing the highly innovative progress in this field, deemed in demand and was fully justified. In order to cover the revolutionary advances in the last decade, Takahiko Akiyama joined as the leading editor in this fourth edition.

In the first and second editions, chiral metal‐based catalysts played the central roles for the asymmetric synthesis because transition‐metal‐catalyzed enantioselective reactions were extensively studied, in particular, in the 1980s and 1990s. Organocatalysis, Lewis and Brønsted acids, C–H activation, carbon‐heteroatom bond forming reactions, and enzyme‐catalyzed reactions were introduced in the third edition.

After 2010, in addition to transition‐metal catalyzed reactions, organocatalysis, including Brønsted acids and C–H activation reactions, has been making remarkable advances. Photoredox catalysis emerged as a useful new synthetic reaction mainly after 2008 and has been rapidly growing and has become a critical methodology. Because the chapters in the third edition are still very informative and the methodologies described therein are still inspiring and stimulating even today, those methodologies are considered “classics” in catalytic asymmetric synthesis.

We decided to edit a new book, which would be the most useful desktop reference book by covering new methodologies, but at the same time keeping the progress in the “classics” of the third edition. In order to capture the most significant progress in the 2010s, several new chapters of organocatalysis are introduced, i.e., enamine and iminium catalysis (Chapter 1), acid catalysis (Chapter 2), base catalysis (Chapter 3), phase transfer catalysis (Chapter 4), peptide catalysis (Chapter 5), carbene catalysis (Chapter 6), and hypervalent catalysis (Chapter 7). Photochemical reactions are also introduced, i.e., photoredox catalysis (Chapter 8), photoredox reactions in the absence of photoredox catalysis (Chapter 9), and [2 + 2] cycloaddition reactions (Chapter 10). The asymmetric C–H bond activation reactions are covered by two chapters, i.e., C(sp²)–H bond (Chapter 11) and C(sp³)–H bond (Chapter 12). Asymmetric halogenation reaction, enzyme‐catalyzed asymmetric synthesis, asymmetric hydrogenation, and asymmetric polymerization are presented in Chapters 13, 14, 15, and 21. The construction of noncentrochiral compounds are discussed in two chapters, i.e., axially chiral compounds (Chapter 19) and planar chiral and helically chiral compounds (Chapter 20). Finally, applications of continuous flow technology to catalytic asymmetric synthesis, which may dramatically change manufacturing processes for pharmaceutical drugs and chiral materials, is discussed in Chapter 21.

We sincerely hope that this book attracts the interest of broad range of synthetic, organic, medicinal, and material chemists, in particular, among the younger generation researchers in both academia and industry, who can bring in creative ideas and innovative approaches to Catalytic Asymmetric Synthesis and advance it to the new height.

Takahiko Akiyama

Iwao Ojima

November, 2021