S,S'-Diethyl dithiomalonate 1 undergoes concomitant alkylation reaction and Michael addition with w-iodo-a,P-unsaturated ketones; the dithiomalonate group present in the cyclization products can be easily reduced by Raney nickel to the ethanol level.$ Iodo enone 10 was prepared from 3-(4-methoxyphenyl)propan-l-o1 according to the following scheme:Reagents and conditions: i, Na, NH3(1);S ii, TsCl, pyridine; iii, 0.1 mol dm-3 HC1; iv, NaI, acetone, reflux 0 The following scheme was used to prepare iodo enone 11. j L &c02..
The absence of effective vaccines for most viral infections highlights an urgent necessity for the design and development of effective antiviral drugs. Due to the advancement in virology since the late 1980s, several key events in the viral life cycle have been well delineated and a number of molecular targets have been validated, culminating in the emergence of many new antiviral drugs in recent years. Inhibitors against enteroviruses and rhinoviruses, responsible for about half of the human common colds, are currently under active investigation. Agents targeted at either viral protein 1 (VP1), a relatively conserved capsid structure mediating viral adsorption/uncoating process, or 3C protease, which is highly conserved among different serotypes and essential for viral replication, are of great potential to become antipicornavirus drugs.
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