Analysis of the reactions used for the preparation of drug candidate molecules.

@article{Carey2006AnalysisOT,
  title={Analysis of the reactions used for the preparation of drug candidate molecules.},
  author={John S. Carey and David Dermot Patrick Laffan and Colin Thomson and Michael Trevelyan Williams},
  journal={Organic \& biomolecular chemistry},
  year={2006},
  volume={4 12},
  pages={
          2337-47
        }
}
The purpose of this perspective is to indicate the range of chemistries used in the manufacture of drug candidate molecules and to highlight certain gaps in current technologies. To do this a survey was carried out of chemical syntheses within the Process Chemistry R&D departments of GlaxoSmithKline, AstraZeneca and Pfizer. 
Applications of Quantum Chemistry in Pharmaceutical Process Development: Current State and Opportunities
TLDR
Application of computational methods to understanding and predicting properties of analogues for drug discovery has enjoyed a long history of success, but the drug development space (post-candidate) has changed significantly. Expand
Simple Preparation of New Potential Bioactive Nitrogen-Containing Molecules and Their Spectroscopy Analysis
The impact of research on the small molecules chemistry is difficult to quantify and currently, it is still one of the most active areas of organic chemistry, medicinal chemistry and lately chemicalExpand
Applying homogeneous catalysis for the synthesis of pharmaceuticals.
  • M. Beller
  • Chemistry, Medicine
  • Ernst Schering Foundation symposium proceedings
  • 2006
This article describes recent achievements of my research group in the Leibniz-Institut für Katalyse e.V. in the area of applied homogeneous catalysis for the synthesis of biologically activeExpand
Large-Scale Applications of Amide Coupling Reagents for the Synthesis of Pharmaceuticals
This review showcases various coupling reagents which have been implemented specifically for large-scale amide synthesis via the condensation of an acid and amine, while highlighting the benefits andExpand
Catalysis: The pharmaceutical perspective
The striking impact of enzymatic and organometallic catalysis on the design of environmentally friendly processes for the discovery and production of pharmaceutical products is discussed. Four caseExpand
Drug discovery chemistry: a primer for the non-specialist.
TLDR
This Foundation Review aims to demystify some of this inherent terminology, providing the non-specialist with a general insight into the nomenclature, terminology and workflow of medicinal chemists within the pharmaceutical industry. Expand
The medicinal chemist's toolbox: an analysis of reactions used in the pursuit of drug candidates.
TLDR
The reaction types used in the pursuit of novel drug candidates are analyzed to evaluate their frequency of occurrence, alongside other factors such as drug likeness, chirality, and the number of steps to each derivative. Expand
Green chemistry tools to influence a medicinal chemistry and research chemistry based organisation
Influencing and improving the environmental performance of a large multi-national pharmaceutical company can be achieved with the help of electronic education tools, backed up by site champions andExpand
1 Biotransformations in Small-molecule Pharmaceutical Development
The demand for medicines that treat illnesses formerly associated with the developed world is expanding at a time when some countries are becoming increasingly affluent. As a result, the globalExpand
Process Development of a Suzuki Reaction Used in the Manufacture of Lanabecestat
We developed a scalable Suzuki process for the synthesis of lanabecestat (+)-camsylate, an active pharmaceutical ingredient that was recently investigated in a Phase III clinical program for theExpand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 53 REFERENCES
Development of a Manufacturing Process for Sibenadet Hydrochloride, the Active Ingredient of Viozan
A process for commercial manufacture of the dual D2-β2 receptor agonist sibenadet hydrochloride has been developed. The process relies upon introduction of operationally simple chemistry at the finalExpand
The Art of Meeting Palladium Specifications in Active Pharmaceutical Ingredients Produced by Pd-Catalyzed Reactions
The use of palladium-derived catalysts in the synthesis of fine chemicals, pharmaceutical inter- mediates and active pharmaceutical ingredients (APIs) has become quite common in the last few dec-Expand
Successful Development and Scale-up of a Palladium-Catalysed Amination Process in the Manufacture of ZM549865
Key steps in the synthesis of ZM549865 (a 5-HT receptor antagonist) are the palladium-catalysed amination of ethyl 8-bromo-6-fluoro-4-oxo-4H-2-chromenecarboxylate and subsequent hydrolysis of theExpand
Industrial methods for the production of optically active intermediates.
TLDR
For the industrial implementation of many transformations alternative methods are available and the advantages of the individual methods will be discussed herein and exemplified by syntheses of relevant compounds. Expand
Application of the chiral base desymmetrisation of imides to the synthesis of the alkaloid jamtine and the antidepressant paroxetine
Abstract The synthesis of the alkaloid jamtine and the antidepressant paroxetine have been addressed by a strategy involving asymmetric desymmetrisation of prochiral imides by a chiral lithium amideExpand
Practical Palladium Catalysts for C-N and C-O Bond Formation
The development of new palladium catalysts for the arylation of amines and alcohols with aryl halides and sulfonates is reviewed. Initial systems as well as mechanistic issues are discussed briefly,Expand
A new synthesis of the GPIIb/IIIa receptor antagonist SB-214857-A
A new synthesis of lotrafiban SB-214857-A is reported. The key steps are the preparation of racemic (4-methyl-3-oxo-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepin-2-yl)-acetic acid methyl ester fromExpand
Enantiospecific synthesis of SB 214857, a potent, orally active, nonpeptide fibrinogen receptor antagonist
Abstract An enantiospecific synthesis of SB 214857, a potent, nonpeplide fibrinogen receptor antagonist, is reported. The synthetic route employs as a key step an intramolecular aryl fluorideExpand
Efficient Fast Screening Methodology for Optical Resolution Agents: Solvent Effects Are Used To Affect the Efficiency of the Resolution Process
An efficient and fast screening methodology for optical resolution agents through the classical crystallization of the corresponding diastereomeric salts is described. In this contribution, weExpand
Efficient synthesis of an imidazole-substituted delta-amino acid by the integration of chiral technologies.
TLDR
Two methods to produce (2S)-5-amino-2-(1-n-propyl-1H-imidazol-4-ylmethyl)-pentanoic acid were investigated and integration of these two approaches via asymmetric hydrogenation of a quinidine salt substrate followed by crystallization provided the desired intermediate in 94% ee and 76% yield. Expand
...
1
2
3
4
5
...