| 摘要 |
NEW MATERIAL:The 2-azetidinone derivative of formula I [R<1> is H, azido or amino; R<2> is 1-4C alkyl, phenyl, p-methylphenyl, p-methoxyphenyl, p-bromophenyl, or benzyl; R<3> is H or SO3(-)M(-) (M(-) is H or cation)]. EXAMPLE:(4R)-(2-Mesyloxythyl)-2-azetidinone. USE:Synthetic intermediate of pharmaceuticals, e.g. azthreonam of formula IIwhich is an antibiotic substance having strong antibacterial activity against Gram-negative bacteria. PROCESS:A compound of formula I wherein R<3> is H can be prepared by reacting the compound of formula III with the organic sulfonyl compound of formula IV(X is Cl or N-imidazolyl) in the presence of a base. The product can be converted to another compound of formula I wherein R<3> is SO3(-)M(-) by reacting with a sulfur trioxide complex. |
