| 摘要 |
<p>PURPOSE:To obtain the subject compound useful as an antibacterial agent on an industrial scale at a low cost by continuously reacting a specific compound with a silylation reagent, an iodination reagent and a specific compound in single reaction vessel. CONSTITUTION:The objective compound of formula IV can be produced by continuously reacting a compound of formula I [R<1> is (protected) amino; R<2> is H or carboxyl-protecting group] with a silylation reagent (e.g., N- trimethylsilylacetamide), an iodination reagent (e.g., iodotrimethylsilane) and a compound of formula II (R<3> is H or trimethylsilyl) in single reaction vessel preferably in an inert solvent (e.g., methylene chloride) and, as necessary, removing the protecting group from the resultant compound of formula III. Preferably, the solubilization reaction is carried out at -10-+50 deg.C for 10-45min and the iodination reaction is carried out by adding 2-6 equivalent of an iodination reagent to the solubilized product under ice cooling and reacting at the above temperature for 0.5-3hr.</p> |
