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

  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},
  volume={4 12},
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

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.

Simple Preparation of New Potential Bioactive Nitrogen-Containing Molecules and Their Spectroscopy Analysis

It is the separation and purification process of the new synthetized organic molecules, the ones that take a key role in drug design and development.

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 and

Applying homogeneous catalysis for the synthesis of pharmaceuticals.

  • M. Beller
  • Chemistry
    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 active

The medicinal chemist's toolbox: an analysis of reactions used in the pursuit of drug candidates.

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.

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, and the pharmaceutical industry is facing increasing pressures that can primarily be attributed to three factors.

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

This review presents a comprehensive overview on selected synthetic routes towards commercial drug compounds as published in both journal and patent literature and focused principally on those drugs containing five-membered heterocycles.

Process Development of a Suzuki Reaction Used in the Manufacture of Lanabecestat

It is reported that the liberated diethanolamine plays an important role in the catalytic process, with supporting evidence for an equilibrium between an unbound and bound palladium complex.



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 final

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-

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 the

Industrial methods for the production of optically active intermediates.

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.

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,

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, we

Efficient synthesis of an imidazole-substituted delta-amino acid by the integration of chiral technologies.

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.

Protecting Groups in Organic Synthesis

Introduction The protection of alcohols The protection of aldehydes and ketones The protection of carboxylic acids The protection of the amino group The protection of thiols The protection of