Automated synthesis: new tools for the organic chemist.

Routine automation of organic chemistry had proved an elusive goal until the arrival of combinatorial chemistry and the economic pressures of increased drug discovery throughput. Now, several approaches have been used to automate chemical synthesis, resulting in a range of new tools, both large and small, to support the process of compound production. The availability of these tools to the organic chemist heralds the change from the traditional 'hand-crafted' philosophy to a more mechanized view of compound synthesis in drug discovery groups.

Novel C-2 substituted carbapenem derivatives. Part III. Synthesis and biological activity of 2-(functionalised ethenyl, oxyiminomethyl and alpha-

The synthesis, antibacterial activity and stability to human dehydropeptidase-1 (DHP-1) of three small series of carbapenems carrying carbon-linked substituents at C-2 are described. C-2 Ethenyl carbapenems showed moderate antibacterial activity but poor stability to DHP-1. C-2 Oxyiminomethyl carbapenems demonstrated variable activity and stability. C-2 alpha-(Hydroxy)benzyl carbapenems were the most promising and showed good potency and DHP-1 stability.