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Heterocyclic Scaffolds (heterocyclic + scaffold)
Selected AbstractsSynthesis of a New Series of Heterocyclic Scaffolds for Medicinal Purposes.CHEMINFORM, Issue 2 2007H. S. Hilal Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Applications of Multicomponent Reactions to the Synthesis of Diverse Heterocyclic ScaffoldsCHEMISTRY - A EUROPEAN JOURNAL, Issue 6 2009James Abstract The sequencing of multicomponent reactions (MCRs) and subsequent cyclization reactions is a powerful stratagem for the rapid synthesis of diverse heterocyclic scaffolds. The optimal MCR is sufficiently flexible that it can be employed to generate adducts bearing a variety of functional groups that may then be selectively paired to enable different cyclization manifolds, thereby leading to a diverse collection of products. The growing interest in diversity-oriented synthesis has led to increased attention to this paradigm for library synthesis, which has inspired many advances in the design and implementation of MCRs for the construction of diverse heterocyclic scaffolds. [source] A Concise and Efficient Synthesis of seco -Duocarmycin SAEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 3 2003Lutz F. Tietze Abstract A short and efficient synthesis of seco -duocarmycin SA (3), a highly potent cytostatic agent and direct precursor of the natural product duocarmycin SA (1), has been achieved. Starting from commercially available 2-methoxy-4-nitroaniline (4) the synthetic protocol contains a Fischer indole synthesis to introduce the heterocyclic scaffold and a radical 5- exo - trig cyclization to furnish the (chloromethyl)indoline ring system as key reactions. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003) [source] Recent Advances in the Synthesis of 2-Imidazolines and Their Applications in Homogeneous CatalysisADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 4 2009Han Liu Abstract As an important class of heterocyclic scaffolds, 2-imidazolines have attracted the attention from the chemists interested in natural products, pharmaceutical chemistry, synthetic organic chemistry, coordination chemistry, and homogeneous catalysis. To fulfill the demand of structural diversity, many efficient methods towards 2-imidazolines, as well as modifications of traditional methods, have been reported in the past two decades. 2-Imidazolines have been developed as ligands in homogeneous catalysis, for the substitution on the nitrogen atom that provides an opportunity for fine-tuning of the electronic effect. This review summarizes recent advances in the synthesis of 2-imidazolines and their applications in homogeneous catalysis. [source] CHARMM general force field: A force field for drug-like molecules compatible with the CHARMM all-atom additive biological force fieldsJOURNAL OF COMPUTATIONAL CHEMISTRY, Issue 4 2010K. Vanommeslaeghe Abstract The widely used CHARMM additive all-atom force field includes parameters for proteins, nucleic acids, lipids, and carbohydrates. In the present article, an extension of the CHARMM force field to drug-like molecules is presented. The resulting CHARMM General Force Field (CGenFF) covers a wide range of chemical groups present in biomolecules and drug-like molecules, including a large number of heterocyclic scaffolds. The parametrization philosophy behind the force field focuses on quality at the expense of transferability, with the implementation concentrating on an extensible force field. Statistics related to the quality of the parametrization with a focus on experimental validation are presented. Additionally, the parametrization procedure, described fully in the present article in the context of the model systems, pyrrolidine, and 3-phenoxymethylpyrrolidine will allow users to readily extend the force field to chemical groups that are not explicitly covered in the force field as well as add functional groups to and link together molecules already available in the force field. CGenFF thus makes it possible to perform "all-CHARMM" simulations on drug-target interactions thereby extending the utility of CHARMM force fields to medicinally relevant systems. © 2009 Wiley Periodicals, Inc. J Comput Chem, 2010 [source] Diketopiperazines in peptide and combinatorial chemistryJOURNAL OF PEPTIDE SCIENCE, Issue 1 2003Dr Peter M. Fischer Abstract Diketopiperazines (DKPs), the smallest cyclic peptides, represent an important class of biologically active natural products and their research has been fundamental to many aspects of peptide chemistry. The advent of combinatorial chemistry has revived interest in DKPs for two reasons: firstly, they are simple heterocyclic scaffolds in which diversity can be introduced and stereochemically controlled at up to four positions; secondly, they can be prepared from readily available ,-amino acids using very robust chemistry. Here synthetic methods, conformation, as well as applications of DKPs are summarized and discussed critically. Copyright © 2003 European Peptide Society and John Wiley & Sons, Ltd. [source] Applications of Multicomponent Reactions to the Synthesis of Diverse Heterocyclic ScaffoldsCHEMISTRY - A EUROPEAN JOURNAL, Issue 6 2009James Abstract The sequencing of multicomponent reactions (MCRs) and subsequent cyclization reactions is a powerful stratagem for the rapid synthesis of diverse heterocyclic scaffolds. The optimal MCR is sufficiently flexible that it can be employed to generate adducts bearing a variety of functional groups that may then be selectively paired to enable different cyclization manifolds, thereby leading to a diverse collection of products. The growing interest in diversity-oriented synthesis has led to increased attention to this paradigm for library synthesis, which has inspired many advances in the design and implementation of MCRs for the construction of diverse heterocyclic scaffolds. [source] A Fluorous, Pummerer Cyclative-Capture Strategy for the Synthesis of N-HeterocyclesCHEMISTRY - A EUROPEAN JOURNAL, Issue 4 2007Laura Abstract A fluorous, cyclative-capture strategy based on a new Pummerer cyclization process allows rapid access to tagged, heterocyclic frameworks. Convenient modification of the fluorous, heterocyclic scaffolds by using a variety of approaches including Pd-catalyzed cross-couplings is possible. Traceless, reductive cleavage of the fluorous-phase tag or oxidative cleavage and further elaboration, completes a strategy for the high-throughput, fluorous-phase synthesis of a diverse range of N-heterocycles. [source] | ||||||||||