Contents: B. Alcaide ∙ P. Almendros: Novel Aspects on the Preparation of Spirocyclic and Fused Unsual β-Lactams.- S.S. Bari ∙ A. Bhalla: Spirocyclic β-Lactams: Synthesis and Biological Evaluation of Novel Heterocycles.- L. Troisi ∙ C. Granito ∙ E. Pindinelli: Novel and Recent Synthesis and Applications of β-Lactams.- C. Palomo ∙ M. Oiarbide: β-Lactams Ring Opening: A Useful Entry to Amino Acids and Relevant Nitrogen-Containing Compounds.- B. Mandal ∙ P. Ghosh ∙ B. Basu: Recent Approaches Towards Solid Phase Synthesis of β-Lactams.- A.Arrieta ∙ B. Lecea ∙ F.P. Cossio: Computational Studies on the Synthesis of β-Lactams Via [ 2+2] Thermal Cycloadditions.- B. K. Banik ∙ I. Banik ∙ F. F. Becker: Novel Anticancer β-Lactams

Richard J. Sundberg Electrophilic Substitution Reactions of Indoles Tara L.S. Kishbaugh Reactions of Indole with Nucleophiles Erin Pelkey Metalation of Indole Jie Jack Li ∙ Gordon W. Gribble Metal-Catalyzed Cross-Coupling Reactions for Indoles Jeanese C. Badenock Radical Reactions of Indole Fariborz Firooznia ∙ Robert F. Kester ∙ Steven J. Berthel [2+2], [3+2] and [2+2+2] Cycloaddition Reactions of Indole Derivatives Robert F. Kester ∙ Steven J. Berthel ∙ Fariborz Firooznia [4+2] Cycloaddition Reactions of Indole Derivatives Jonathon S. Russel Oxindoles and Spirocyclic Variations: Strategies for C3 Functionalization Liangfeng Fu Advances in the Total Syntheses of Complex Indole Natural Products

This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Key Heterocycle Cores for Designing Multitargeting Molecules provides a helpful overview of current developments in the field. Following a detailed introduction to the manipulation of heterocycle cores for the development of dual or multitargeting molecules, the book goes on to describe specific examples of such developments, focusing on compounds such as Benzimidazole, Acridine, Flavones, Thiazolidinedione and Oxazoline. Drawing on the latest developments in the field, this volume provides a valuable guide to current approaches in the design and development of molecules capable of acting on multiple targets. Adapting the heterocyclic core of a single-target molecule can facilitate its development into an agent capable of acting on multiple targets. Such multi-targeting drugs have the potential to become essential components in the design of novel, holistic treatment plans for complex diseases, making the design of such active agents an increasingly important area of research. - Emphasizes the chemical development of heterocyclic nuclei, from single to multitargeting molecules - Provides chapter-by-chapter coverage of the key heterocyclic compounds used in synthesizing multitargeting agents - Outlines current trends and future developments in multitarget molecule design for the treatment of various diseases

Carbon-carbon and carbon-heteroatom bond-forming reactions are the backbone of synthetic organic chemistry. Scientists are constantly developing and improving these techniques in order to maximize the diversity of synthetically available molecules. These techniques must be developed in a sustainable manner in order to limit their environmental impact. This book highlights green bond forming reactions for bioactive scaffolds.

Abstract: Small, polyfunctionalized heterocycles have attracted significant attention in the design of biologically active compounds in the drug discovery enterprise. Research in the area of combinatorial synthesis employing heterocycles as scaffolds for library development has become very prominent. Pyridine-containing heterocycles, such as tetrahydronaphthyridines, have been shown to possess a variety of biologic activities. Previous work in our group developed an inverse-electron-demand Diets-Alder (IEDDA) strategy to prepare the 1,2,3,4-tetrahydro-1,5-naphthyridines, however, the preparation of the other tetrahydronaphthyridine analogues could not be achieved via this IEDDA strategy. Thus, metal-catalyzed [2 + 2 + 2] cyclizations between a nitrite and two alkynes were investigated in both intermolecular and intramolecular reactions, which have the potential to prepare all the tetrahydronaphthyridine isomers. To determine optimal conditions, different transition metals (Co, Zr, Ni, Ir, Ru, and Au), as well as reaction conditions (thermal heating, photochemical activation, and microwave irradiation) were screened. The best results were achieved when CpCo(CO) 2 was employed as catalyst, under microwave irradiation in chlorobenzene. Using the optimized microwave-promoted conditions, the intermolecular cyclizations between amino alkynyl nitriles and alkynes gave the desired 5,6,7,8-tetrahydro-1,6-naphthyridines in modest yields, while the intramolecular cyclizations of dialkynyl aminonitrile precursors afforded dihydropyran ring-fused tetrahydronaphthyridines in excellent yields. Finally, a heterocyclic natural product, naringenin, was investigated for its suitability as a library scaffold. Belonging to the flavonone class, naringenin is characterized by the rigid tricyclic benzopyran core with three phenols at C-5, C-7 and C-4' positions. Recent epidemiological studies showed increasing evidence for the anticancer and antiatherogenic properties of this natural product. Its rigid, densely functionalized tricyclic scaffold is an attractive structure for discovering novel bioactive molecules. Thus, suitable chemistries were explored on these scaffolds in an effort to define regioselective transformations of the phenolic groups through palladium catalyzed cross-coupling chemistry which could be applied to library development.