In the series of Topics in Heterocyclic Chemistry, the volume of Bioactive Heterocycles aims to present comprehensive reviews on selected topics of synthetic as well as naturally occurringbioactive heterocycles.

The present volume comprises six chapters of the following specialized reviews.

The first chapter, 'Directed Synthesis of Biologically Interesting Heterocycles with Squaric Acid Based Technology' by Masatomi Ohno and Shoji Eguchi covers squaric acid and its derivatives as versatile synthons for target-oriented and diversity-oriented synthesis. The introduction of designed functional groups, followed by ring conversion induced thermally or by reactive intermediates can construct a various bioactive heterocycles including bioactive natural products.

The second chapter 'Manganese(III)-Based Peroxidation of Alkenes to Heterocycles' by Hiroshi Nishino presents a very comprehensive review on novel Mn(III)-based peroxidation chemistry, and related bioactive heterocycles based on the works of his group. The content includes synthesis of functionalized 1,2-dioxane derivatives from various 1,3-dicarbonyl compounds including nitrogen heterocycles. The spectroscopic feature, the formation mechanism of 1,2-dioxan-3-ol ring system, chemical transformations and synthetic applications are also discussed.

The third chapter 'A Frontier in Indole Chemistry: 1-Hydroxyindoles, 1-Hydroxytryptamines, and 1-Hydroxytryptophans' by Masanori Somei presents a very comprehensive review on chemistry of 1 -hydroxy-indoles, -tryptamines, and -tryptophans as a frontier in indole chemistry. In fact, these new members of indole derivatives were not much known about 30 years ago in the long histry of indole alkaloids and related chemistry. Nowadays, these new families of indole compounds have been demonstrated to play their important role in life and nature by the pioneering works of Somei and his coworkers. The interesting biological and pharmaceutical activities have been found in these derivatives.

The fourth chapter 'Quinazoline Alkaloids and Related Chemistry' by Shoji Eguchi provides a perspective review focusing on developements of the synthetic methodologies and their synthetic applications. A brief historical background, aza-Wittig methodology, microwave-assisted synthesis, solid-phase synthesis, and a variety of new synthesis of quinazoline compounds by organo-metallic reagents, metal-catalyzed reactions, heterocyclizations, pericyclic reactions etc are briefly reviewed. Selected topics of total synthesis of various types of quinazoline alkaloids including substituted type like febrifugine and heterocycle-fused type such as pyrroloquinazolines, indolopyridoquinazo-lines, pyrazinoquinazolines, pyrroloquinazolinoquinolines by these methodologies are discussed.

The fifth chapter 'Bioactive Heterocyclic Alkaloids from Marine Orgin' by Masakin Kita and Daisuke Uemura presents a very comprehensive review on novel heterocyclic marine alkaloids with very intriguing structures and useful biological properties like anti-osteoprotic activity focusing on isolations, structural, synthetic, biological, and biogenetic studies mainly by Uemura group. The contents are believed to attract much attention by organic chemists, hetero-cyclic chemists, synthetic chemists, and workers in medicinal, pharmaceutical and bioscience fields.

The sixth chapter 'Synthetic Studies on Heterocyclic Antibiotics Containing Nitrogen Atoms' by Hiromasa Kiyota presents a very comprehensive review on a variety of heterocyclic antibiotics and phytotoxins. Early and recent examples of synthetic studies of glutarimide antibiotics, antimycins, and tabtoxins and related bioactive heterocycles based on the works of his group are retrospectively reviewed. The content is believed to attracts much interest of synthetic chemists as well as heterocyclic chemists and researchers in life science fields.

I hope that our readers find this series to be a useful guide to modern hete-rocyclic chemistry. As always, I encourage both suggestions for improvements and ideas for review topics.

Nagoya, March 2006 Shoji Eguchi

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