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Produktbild: Signposts to Chiral Drugs
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Signposts to Chiral Drugs Organic Synthesis in Action

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Beschreibung

Produktdetails

Einband

Taschenbuch

Erscheinungsdatum

21.09.2014

Verlag

Birkhäuser Basel

Seitenzahl

232

Maße (L/B/H)

23,5/15,5/1,4 cm

Gewicht

388 g

Auflage

2011

Sprache

Englisch

ISBN

978-3-0348-0770-8

Beschreibung

Rezension

From the reviews:

"In this timely book, Sunjic and Parnham provide an exciting selection of major achievements in drug development and unfold 15 intriguing success stories of aliskiren, vancomycin, paclitaxel, menthol, efavirenz, and others from the perspective of a medicinal chemist. ... This book will be most appealing to undergraduate and graduate students with an interest in synthesis and stereochemistry ... . it should be considered an instructive teaching supplement that underscores the general significance and impact of creative synthetic chemistry and stimulates further discussion in the classroom." (Christian Wolf, Journal of the American Chemical Society, September, 2011)

"The subject of the book are chiral drugs. ... Each chapter can be read separately and consists of an abstract, introduction, the main part with the synthetic approach to a certain drug, conclusion and references. ... References are relevant and up-to date. A long list of abbreviations and acronyms is provided at the beginning ... . The book will be very useful to synthetic organic and medicinal chemists in innovative pharmaceutical companies and to scientists and ambitious students of chemistry and pharmacy." (Branka Zorc, Acta Pharmaceutica, Vol. 61, 2011)

"This ... volume will be of interest to those working in synthetic organic chemistry, particularly in the medicinal chemistry area, and having as their aim the discovery of new drug entities for the pharmaceutical industries. ... there is also a useful summary of synthetic methods and concepts that are developed in the individual chapters, together with a useful index. The standard of presentation is very high, with many clearly presented reaction schemes, and each chapter has a comprehensive list of references to the specific area." (D. W. Allen, Inflammopharmacology, Vol. 19, 2011)

Produktdetails

Einband

Taschenbuch

Erscheinungsdatum

21.09.2014

Verlag

Birkhäuser Basel

Seitenzahl

232

Maße (L/B/H)

23,5/15,5/1,4 cm

Gewicht

388 g

Auflage

2011

Sprache

Englisch

ISBN

978-3-0348-0770-8

Herstelleradresse

Springer-Verlag GmbH
Tiergartenstr. 17
69121 Heidelberg
DE

Email: ProductSafety@springernature.com

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  • Produktbild: Signposts to Chiral Drugs
  • 1. Organic synthesis in drug discovery and development
    1.      Introduction
    2.      Synthetic organic chemistry in drug R&D process
    3.      New concepts in drug discovery process
             3.1.   The impact of natural products upon modern drug discovery
    3.2.    Biology oriented and DNA-templated synthesis in drug discovery
             3.3.   Incorporation of genomics in drug discovery
    4.      Conclusion
    References
    2. Aliskiren fumarate
     
    1.                 Introduction
    2.            Renin and the mechanism of action of aliskiren
    3.            Structural characteristics and synthetic approaches to aliskiren
    3.1       Strategy based on visual imagery, starting from Nature’s chiral pool; a Dali-like presentation of objects
    3.2 Fine-tuning of the chiral ligand for the Rh complex; hydrogenation of the selected substrate with extreme enantioselectivities
    4.            Conclusion
    References
     
    3. (R)-K-13675
    3.1   Introduction
    3.2   Peroxisome proliferator-activated receptor a (PPARa) agonists.
    3.2.1 b-Phenylpropionic acids
    3.2.2 a-Alkoxy-b-arylpropionic acids
    3.2.3 a-Aryloxy-b-phenyl propionic acids.
    3.2.4 Oxybenzoylglycine derivatives.
    3.3 Non-hydrolytic anomalous lactone ring-opening
    3.4 Mitsunobu reaction in the ether bond formation
    3.5 Conclusion
    References
     
    4. Sitagliptin phosphate monohydrate
    4.1 Introduction
    4.2 Endogenous glucoregulatory peptide hormones and dipeptidyl peptidase IV (DPP4) inhibitors
    4.3 Synthesis with C-acyl mevalonate as the N-acylating agent
    4.4   Highly enantioselective hydrogenation of unprotected b-enamino amides and the use of Josiphos-ligands
    4.5 Ammonium chloride, an effective promoter of catalytic enantioselective hydrogenation
    4.6 Conclusion
    References
     
    5. Biaryl unit in valsartan and vancomycin 
    5.1 Introduction
    5.2   Angiotensin AT1 receptor, G-protein coupled receptors (GPCRs).
    5.3 Cu-promoted catalytic decarboxylative biaryl synthesis, biomimetic type aerobic decarboxylation
    5.4 Stereoselective approach to axially chiral biaryl system; the case of vancomycin
    5.5 Conclusion
    References
     
    6. 3-Amino-1,4-benzodiazepines
    6.1 Introduction
    6.2 3-Amino-1,4-benzodiazepine derivatives, g-secretase inhibitors
    6.3 Configurational stability; racemization and enantiomerization
    6.4 Crystallization induced asymmetric transformation
    6.5 Asymmetric Ireland-Cleisen rearrangement
    6.6 Hydroboration of the terminal C=C bond; anti-Markovnikov hydratation
    6.7 Crystallization-induced asymmetric transformation in the synthesis of L-768,673
    6.8 Conclusion
    References
     
    7. Sertraline
    7.1 Introduction
    7.2 Synaptosomal serotonin uptake and its selective inhibitors (SSRI)
    7.3 Action of sertraline and its protein target
    7.4 General synthetic route
    7.5 Stereoselective reduction of ketones and imines under kinetic and thermodynamic control
    7.5.1 Diastereoselectivity of hydrogenation of rac-tetralone-methylimine; the old (MeNH2/TiCl4/toluene) method is improved by using MeNH2/EtOH-Pd/CaCO3, 60-65 oC in a telescoped process
    7.5.2 Kinetic resolution of racemic methylamine; hydrosylilation by (R,R)-(EBTHI)TiF2 /PhSiH3 catalytic system
    7.5.3 Catalytic epimerization of the trans- to the cis-isomer of sertraline
    7.5.4 Stereoselective reduction of tetralone by chiral diphenyloxazaborolidine
    7.6. Desymmetrization of oxabenzonorbornadiene, Suzuki coupling of arylboronic acids and vinyl halides
    7.7 Pd-Catalyzed (Tsuji-Trost) coupling of arylboronic acids and allylic esters
    7.8 Simulated moving bed (SMB) in the commercial production of sertraline
    7.9 Conclusion
    References
     
    8. 1,2-Dihydroquinolines
    8.1 Introduction8.2       Glucocorticoid receptor (GCR)
    8.3 Asymmetric organocatalysis; introducing a thiourea catalyst for Petasis   reaction
    8.3.1 General consideration of the Petasis reaction
    8.3.2 Catalytic,  enantioselective Petasis reaction
    8.4 Multicomponent reactions (MCRs); general concept and examples
    8.4.1 General concept of MCRs
    8.4.2 Efficient, isocyanide-based Ugi MCRs
    8.5 Conclusion
    References
     
    9. (-)-Menthol
    9.1 Introduction
    9.2. Natural sources and first technological production of (-)-menthol
    9.3   Enantioselective allylic amine-enamine-imine rearrangement, catalysed by Rh(I)-(-)-BINAP complex.9.4 Production scale synthesis of both enantiomers
    9.5 Conclusion
    References
     
    10. Fexofenadine hydrochloride
    10.1 Introduction
    10.2 Histamine receptors as biological targets for antiallergy drugs
    10.3 Absolute configuration and “racemic switch”
    10.4 Retrosynthetic analysis of fexofenadine
    10.4.1 ZnBr2-Catalyzed rearrangement of a-haloketones to terminal carboxylic acids
    10.4.2 Microbial oxidation of non-activated C-H bond.
    10.4.3 Bioisosterism; silicon switch of fexofenadine to sila-fexofenadine
    10.5 ConclusionReferences
     
    11. Montelukast sodium
    11.1 Introduction
    11.2 Leukotriene D4 receptor (LTD4), CysLT-1 receptor, antagonists
    11.3 Hydroboration of ketones with boranes from ?-pinenes and the non-linear effect (NLE) in asymmetric reactions
    11.4 Ru(II) catalyzed enantioselective hydrogen transfer
    11.5 Biocatalytic reduction with ketoreductase KRED (KetoREDuctase)
    11.6 CeCl3-THF solvate as a promoter of the Grignard reaction; phase transfer catalysis
    11.7 Conclusion
    References
     
    12. Thiolactone peptides as antibacterial peptidomimetics
    12.1. Introduction
    12.2 Virulence and quorum sensing system of Staphylococcus aureus.12.3 Development of chemical ligation (CL) in peptide synthesis
    12.4  Development of native chemical ligation (NCL); chemoselectivity in peptide synthesis
    12.5  Development of NCL  in thiolactone peptide synthesis
    12.6 Conclusion
    References
     
    13. Efavirenz
    13.1 Introduction
    13.2 HIV-1 reverse transcriptase (RT) inhibitors
    13.2.1 Steric interactions at the active site
    13.3 Asymmetric addition of alkyne anion to C=O bond with formation of chiral Li+ aggregates
    13.3.1 Mechanism of the chirality transfer
    13.3.2 Equilibration of lithium aggregates and the effect of their relative stability on enantioselectivity
    13.4 Scale-up of alkynylation promoted by the use of Et2Zn. 
    13.5 Conclusion
    References
     
    14. Paclitaxel
    14.1 Introduction
    14.2 Disturbed dynamics of cellular microtubules by binding to ß-tubulin
    14.2  Three selected synthetic transformations on the pathway to paclitaxel
    14.3 Three selected synthetic transformations on the pathway to paclitaxel
    14.3.1 Intramolecular Heck reaction on the synthetic route to baccatin III
    14.3.2 Trifunctional catalyst for biomimetic synthesis of chiral diols; synthesis of the paclitaxel side-chain
    14.3.3 Zr-complex catalysis in the reductive N-deacylation of taxanes to the primary amine, the key precursor of paclitaxel
    14.4 Conclusion
    References
     
    15. Neoglycoconjugate
    15.1 Introduction
    15.2 Human a-1,3-fucosyltransferase (Fuc-T)
    15.3 Click chemistry, energetically preferred reactions
    15.4 Target-guided synthesis (TGS) or freeze-frame click chemistry
    15.5 Application of click chemistry to the synthesis of nucleoconjugate 1
    15.6 Conclusion
    References
     
    16. 12-Aza epothilones
    16.1 Introduction
    16.2 Epothilones; mechanism of action and structure-activity relationships
    16.3. Extensive versus peripheral structural modifications of natural products
    16.4  Ring closure metathesis (RCM), an efficient  approach to mac rocyclic “non-natural natural-products”
    16.5Diimide reduction of the allylic C=C bond
    16.6Conclusion
    References