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.

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

Asymmetric Synthesis of Active Pharmaceutical Ingredients

Throughout the past two decades, the relationship between chirality and biological activity has become an area of vital importance to medicinal chemists in both the design and synthesis of novel small molecules. In this chapter, the definition of chirality and its biological implications are covered. The synthetic, chromatographic, and crystallization approaches to single isomer compounds are discussed with reference to the differing biological activities exhibited by stereoisomers.


Keywords:

chirality;
stereoisomers;
asymmetric;
resolution/separation;
drug;
binding;
potency;
metabolism

Chirality and Biological Activity

A simple and efficient stereoselective synthesis of (R)-denopamine and other naturally occurring hydroxy amides from optically active (R)-2-azido-1-arylethanols, is described for the first time via reduction of the corresponding α-azidoarylketones with enzymes from Daucus Carota root, under mild and environmentally friendly conditions. The products are formed with high degrees of enantioselectivity.

Stereoselective synthesis of (R)-(−)-denopamine, (R)-(−)-tembamide and (R)-(−)-aegeline via asymmetric reduction of azidoketones by Daucus carota in aqueous medium

Biocatalytic hydrogen-transfer reduction of α-chloro-ketones furnished non-racemic chlorohydrins by employing either Rhodococcus ruber as lyophilized cell catalyst or an alcohol dehydrogenase preparation from Pseudomonas fluorescens DSM 50106 (PF-ADH). For all substrates investigated, Rhodococcus ruber gave strictly the “Prelog” product, whereas PF-ADH showed scattered stereopreference. One possibility for a follow-up reaction of halohydrins is the ring closure to the corresponding epoxide. A novel “one pot-one step strategy” was employed to obtain the enantiopure epoxide from the α-chloro-ketone in a cascade like fashion at pH>12 involving biocatalytic hydrogen transfer reduction and in situ chemo-catalyzed ring closure.

Non-Racemic Halohydrins via Biocatalytic Hydrogen-Transfer Reduction of Halo-Ketones and One-Pot Cascade Reaction to Enantiopure Epoxides

An efficient enantioselective route to ( S )-salmeterol involving asymmetric reduction of an azidoketone intermediate to an azido alcohol by Pichia angusta is described.

Enantioselective synthesis of (S)-salmeterol via asymmetric reduction of azidoketone by Pichia angusta

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Enantioselective synthesis of (S)-salmeterol via asymmetric reduction of azidoketone by Pichia angusta