George William Hardy

β-Anomer selectivity in 2′-deoxynucleoside synthesis: A novel approach using an acyl carbamate directing group

Abstract Glycosylation of silylated pyrimidines using a phenyl 2-deoxy-3- O -( N -benzoyl)carbamoyl-1-thio-D-erythro-pentofuranoside yielded 2-deoxy-β- ribo nucleosides in good yields with excellent anomeric selectivity. This prototype 3- O -carbamate directing group was readily formed and removed in high yields.

Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma

The discovery of a novel series of therapeutic agents that has been designed and optimized for treating chronic obstructive pulmonary disease is reported. The pharmacological strategy was based on the identification of compounds that inhibit a defined subset of kinase enzymes modulating inflammatory processes that would be effective against steroid refractory disease and exhibit a sustained duration of action after inhaled delivery.

ACYL CARBAMATE DIRECTING GROUPS IN NUCLEOSIDE SYNTHESIS : APPLICATIONS IN THE SYNTHESIS OF 2'-DEOXY-5-ETHYL-4'-THIOURIDINE

Abstract The use of the 3- O -( N -acyl)carbamoyl directing groups in the synthesis of the potent anti-Herpes virus agent 2′-deoxy-5-ethyl-4′-thio-D-uridine is described. This includes details of experiments to optimise the carbamate substitution and a multi-gram exemplification of the key steps.