Michael Trevelyan Williams

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.

A highly selective N-protection strategy for the preparation of 1-N-alkylated kanamycin antibiotics

Abstract An O to N acyl migration technique has been used to selectively acetylate the amino groups of the aminosugar rings of kanamycins A and B, leaving the amino groups on the 2-deoxy-streptamine ring unprotected. A formylation-deformylation process then converts these N-acetylated kanamycins to their 3-N-formyl derivatives with high regioselectivity, giving key intermediates for the efficient preparation of 1-N-alkylated kanamycins.