David Dermot Patrick Laffan

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

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.

Studies in macrolide synthesis: a concise asymmetric synthesis of a macrolide intermediate for the erythronolides

Abstract The enantiomerically-pure 14-membered ring macrolide 1 is prepared in 14 steps from the racemic aldehyde 4, Z=SPh. The C2-C4 and C8-C10 stereorelationships in 1 are controlled in a single step by an Evans aldol condensation with (±)-4. Macrolactonisation, 23 → 1, takes place in high yield (91%).